Search and Browse
Download
Enter Data
Search by PubMed Identification
| PMID | Data | Article Title | Citation | Organization | Data Download |
|---|---|---|---|---|---|
| 12963436 | 3 | Interactions of glycyrrhizin with organic anion transporting polypeptides of rat and human liver. |
Hepatol Res 26: 343-347 (2003) | University of Zurich | 2D 3D TSV |
| 12954816 | 2 | N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. |
J Pharmacol Exp Ther 307: 322-30 (2003) | Novartis Pharma AG | 2D 3D TSV |
| 12954796 | 58 | In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates. |
J Pharmacol Exp Ther 307: 138-45 (2003) | National Institute on Drug Abuse | 2D 3D TSV |
| 12954329 | 8 | The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity. |
Chem Biol 10: 705-12 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12954072 | 46 | New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity. |
J Med Chem 46: 4196-204 (2003) | Georgetown University Medical Center | 2D 3D TSV |
| 12954071 | 109 | A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. |
J Med Chem 46: 4188-95 (2003) | Alcon Research Ltd | 2D 3D TSV |
| 12954070 | 24 | Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic. |
J Med Chem 46: 4182-7 (2003) | University of Innsbruck | 2D 3D TSV |
| 12954066 | 63 | In vitro analysis of stable, receptor-selective neurotensin[8-13] analogues. |
J Med Chem 46: 4141-8 (2003) | Medical University of South Carolina | 2D 3D TSV |
| 12954065 | 8 | Orally active oxime derivatives of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one. Synthesis and pharmacological activity. |
J Med Chem 46: 4136-40 (2003) | University Center for Pharmacy | 2D 3D TSV |
| 12954062 | 140 | 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators. |
J Med Chem 46: 4104-12 (2003) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
| 12954061 | 153 | Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids. |
J Med Chem 46: 4087-103 (2003) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
| 12954060 | 4 | CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
J Med Chem 46: 4070-86 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12954059 | 55 | Selectivity fields: comparative molecular field analysis (CoMFA) of the glycine/NMDA and AMPA receptors. |
J Med Chem 46: 4063-9 (2003) | Moscow State University | 2D 3D TSV |
| 12954058 | 193 | Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. |
J Med Chem 46: 4050-62 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12954057 | 113 | Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors. |
J Med Chem 46: 4043-9 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12954056 | 14 | Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process. |
J Med Chem 46: 4032-42 (2003) | Università di Pisa | 2D 3D TSV |
| 12954055 | 47 | Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. |
J Med Chem 46: 4021-31 (2003) | Johnson and Johnson Pharmaceutical Research and Development | 2D 3D TSV |
| 12954053 | 39 | Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2. |
J Med Chem 46: 4002-8 (2003) | University of Maryland | 2D 3D TSV |
| 12954052 | 25 | Synthesis and SAR of thrombin inhibitors incorporating a novel 4-amino-morpholinone sscaffold: analysis of X-ray crystal structure of enzyme inhibitor complex. |
J Med Chem 46: 3985-4001 (2003) | Link£ping University | 2D 3D TSV |
| 12954051 | 10 | Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation. |
J Med Chem 46: 3975-84 (2003) | Dr. Reddy's Laboratories Ltd | 2D 3D TSV |
| 12954050 | 2 | Receptor-mediated targeting of a photosensitizer by its conjugation to gonadotropin-releasing hormone analogues. |
J Med Chem 46: 3965-74 (2003) | Institute of Science | 2D 3D TSV |
| 12954049 | 2 | Discovery and preclinical characterization of (+)-3-[4-(1- piperidinoethoxy)phenyl]spiro[indene- 1,1'-indane]-5,5'-diol hydrochloride: a promising nonsteroidal estrogen receptor agonist for hot flush. |
J Med Chem 46: 3961-4 (2003) | Dainippon Pharmaceutical Co., Ltd. | 2D 3D TSV |
| 12954048 | 36 | The first potent and selective non-imidazole human histamine H4 receptor antagonists. |
J Med Chem 46: 3957-60 (2003) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12954047 | 80 | Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. |
J Med Chem 46: 3953-6 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12951129 | 30 | Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists. |
Bioorg Med Chem Lett 13: 3375-9 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12951128 | 51 | Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists. |
Bioorg Med Chem Lett 13: 3371-4 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12951127 | 32 | Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists. |
Bioorg Med Chem Lett 13: 3367-70 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12951126 | 39 | Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1). |
Bioorg Med Chem Lett 13: 3361-5 (2003) | Berlex Biosciences | 2D 3D TSV |
| 12951125 | 18 | N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates. |
Bioorg Med Chem Lett 13: 3355-9 (2003) | Virginia Commonwealth University | 2D 3D TSV |
| 12951124 | 2 | Stereoselective synthesis of phosphoramidate alpha(2-6)sialyltransferase transition-state analogue inhibitors. |
Bioorg Med Chem Lett 13: 3351-4 (2003) | Universitaet Konstanz | 2D 3D TSV |
| 12951122 | 20 | Further SAR studies on novel small molecule inhibitors of the hepatitis C (HCV) NS5B polymerase. |
Bioorg Med Chem Lett 13: 3341-4 (2003) | Shire BioChem Inc | 2D 3D TSV |
| 12951120 | 32 | Alpha-keto amides as inhibitors of histone deacetylase. |
Bioorg Med Chem Lett 13: 3331-5 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12951118 | 24 | HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent. |
Bioorg Med Chem Lett 13: 3323-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12951117 | 31 | Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor. |
Bioorg Med Chem Lett 13: 3317-22 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12951116 | 30 | Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists. |
Bioorg Med Chem Lett 13: 3311-5 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12951114 | 18 | Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors. |
Bioorg Med Chem Lett 13: 3301-3 (2003) | University of California | 2D 3D TSV |
| 12951113 | 11 | Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase. |
Bioorg Med Chem Lett 13: 3297-300 (2003) | McGill University/Royal Victoria Hospital | 2D 3D TSV |
| 12951112 | 150 | Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid. |
Bioorg Med Chem Lett 13: 3293-6 (2003) | Friedrich-Alexander University | 2D 3D TSV |
| 12951108 | 63 | Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression. |
Bioorg Med Chem Lett 13: 3277-80 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12951107 | 8 | Synthesis and PDF inhibitory activities of novel benzothiazolylidenehydroxamic acid derivatives. |
Bioorg Med Chem Lett 13: 3273-6 (2003) | Senju Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12951102 | 46 | Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor. |
Bioorg Med Chem Lett 13: 3247-52 (2003) | Purdue Pharma LP | 2D 3D TSV |
| 12951101 | 79 | Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors. |
Bioorg Med Chem Lett 13: 3243-6 (2003) | Pfizer Inc | 2D 3D TSV |
| 12951100 | 6 | Cyclohexanedione herbicides are inhibitors of rat heart acetyl-CoA carboxylase. |
Bioorg Med Chem Lett 13: 3237-42 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12951099 | 28 | Bisphosphonates derived from fatty acids are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase. |
Bioorg Med Chem Lett 13: 3231-5 (2003) | Universidad de Buenos Aires | 2D 3D TSV |
| 12951093 | 12 | Design and synthesis of dimeric HIV-1 integrase inhibitory peptides. |
Bioorg Med Chem Lett 13: 3203-5 (2003) | NIH | 2D 3D TSV |
| 12951091 | 36 | Design and synthesis of fluorinated RXR modulators. |
Bioorg Med Chem Lett 13: 3191-5 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12951090 | 57 | O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists. |
Bioorg Med Chem Lett 13: 3185-90 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12951089 | 13 | Regulation of gene expression by synthetic dimerizers with novel specificity. |
Bioorg Med Chem Lett 13: 3181-4 (2003) | ARIAD Gene Therapeutics, Inc. | 2D 3D TSV |
| 12951088 | 22 | Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands. |
Bioorg Med Chem Lett 13: 3177-80 (2003) | Universidad Complutense | 2D 3D TSV |
| 12951087 | 23 | Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics. |
Bioorg Med Chem Lett 13: 3171-6 (2003) | University of Ljubljana | 2D 3D TSV |
| 12951085 | 10 | Reversed hydroxamate-bearing thermolysin inhibitors mimic a high-energy intermediate along the enzyme-catalyzed proteolytic reaction pathway. |
Bioorg Med Chem Lett 13: 3161-6 (2003) | Pohang University of Science and Technology | 2D 3D TSV |
| 12951084 | 8 | 1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists. |
Bioorg Med Chem Lett 13: 3155-9 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12951083 | 12 | Biological activities of alpha-mangostin derivatives against acidic sphingomyelinase. |
Bioorg Med Chem Lett 13: 3151-3 (2003) | Keio University | 2D 3D TSV |
| 12951082 | 10 | Analysis of the critical structural determinant(s) of species-selective peroxisome proliferator-activated receptor alpha (PPAR alpha)-activation by phenylpropanoic acid-type PPAR alpha agonists. |
Bioorg Med Chem Lett 13: 3145-9 (2003) | Kyorin Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12951078 | 38 | Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors. |
Bioorg Med Chem Lett 13: 3129-32 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12946343 | 3 | The 1.15A crystal structure of the Staphylococcus aureus methionyl-aminopeptidase and complexes with triazole based inhibitors. |
J Mol Biol 332: 13-21 (2003) | Morphochem AG | 2D 3D TSV |
| 12941345 | 42 | Potent small molecule inhibitors of spleen tyrosine kinase (Syk). |
Bioorg Med Chem Lett 13: 3111-4 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12941344 | 18 | Mapping the kinase domain of Janus Kinase 3. |
Bioorg Med Chem Lett 13: 3105-10 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12941343 | 49 | The kinetics of binding to p38MAP kinase by analogues of BIRB 796. |
Bioorg Med Chem Lett 13: 3101-4 (2003) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
| 12941342 | 21 | Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor. |
Bioorg Med Chem Lett 13: 3097-100 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12941341 | 23 | Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent. |
Bioorg Med Chem Lett 13: 3091-5 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12941340 | 10 | Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue. |
Bioorg Med Chem Lett 13: 3087-90 (2003) | Scios Inc | 2D 3D TSV |
| 12941339 | 23 | 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK). |
Bioorg Med Chem Lett 13: 3083-6 (2003) | University of Newcastle | 2D 3D TSV |
| 12941338 | 18 | Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. |
Bioorg Med Chem Lett 13: 3079-82 (2003) | University of Newcastle | 2D 3D TSV |
| 12941336 | 7 | Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents. |
Bioorg Med Chem Lett 13: 3071-4 (2003) | ARIAD Pharmaceuticals Inc | 2D 3D TSV |
| 12941335 | 8 | Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases. |
Bioorg Med Chem Lett 13: 3067-70 (2003) | ARIAD Pharmaceuticals Inc | 2D 3D TSV |
| 12941334 | 22 | Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues. |
Bioorg Med Chem Lett 13: 3063-6 (2003) | ARIAD Pharmaceuticals Inc | 2D 3D TSV |
| 12941333 | 61 | 6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). |
Bioorg Med Chem Lett 13: 3059-62 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12941332 | 27 | 6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
Bioorg Med Chem Lett 13: 3055-7 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12941331 | 96 | Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. |
Bioorg Med Chem Lett 13: 3049-53 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12941330 | 30 | Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
Bioorg Med Chem Lett 13: 3045-8 (2003) | Ghent University | 2D 3D TSV |
| 12941329 | 30 | Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity. |
Bioorg Med Chem Lett 13: 3041-4 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12941327 | 24 | Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. |
Bioorg Med Chem Lett 13: 3031-4 (2003) | Wyeth Research | 2D 3D TSV |
| 12941326 | 26 | Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides. |
Bioorg Med Chem Lett 13: 3027-30 (2003) | Instituto de Química Médica (CSIC) | 2D 3D TSV |
| 12941325 | 18 | Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation. |
Bioorg Med Chem Lett 13: 3021-6 (2003) | AstraZeneca | 2D 3D TSV |
| 12941324 | 66 | Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes. |
Bioorg Med Chem Lett 13: 3015-9 (2003) | Kyoto University | 2D 3D TSV |
| 12941322 | 12 | Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration. |
Bioorg Med Chem Lett 13: 3005-7 (2003) | NIH | 2D 3D TSV |
| 12941321 | 40 | Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. |
Bioorg Med Chem Lett 13: 3001-4 (2003) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
| 12941319 | 15 | 2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors. |
Bioorg Med Chem Lett 13: 2993-6 (2003) | Academy of Sciences of the Czech Republic | 2D 3D TSV |
| 12941318 | 46 | Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors. |
Bioorg Med Chem Lett 13: 2989-92 (2003) | Academy of Sciences of the Czech Republic | 2D 3D TSV |
| 12941317 | 25 | Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis. |
Bioorg Med Chem Lett 13: 2985-8 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12941316 | 9 | Synthesis of three enantiomeric pairs of scyllo-inositol phosphate and molecular interactions between all possible regioisomers of scyllo-inositol phosphate and inositol 1,4,5-trisphosphate 3-kinase. |
Bioorg Med Chem Lett 13: 2981-4 (2003) | Pohang University of Science & Technology | 2D 3D TSV |
| 12941315 | 19 | Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines. |
Bioorg Med Chem Lett 13: 2977-80 (2003) | Wyeth Research | 2D 3D TSV |
| 12941314 | 17 | Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors. |
Bioorg Med Chem Lett 13: 2973-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12941313 | 20 | Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. |
Bioorg Med Chem Lett 13: 2967-71 (2003) | Novartis Pharma AG | 2D 3D TSV |
| 12941312 | 58 | Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines. |
Bioorg Med Chem Lett 13: 2961-6 (2003) | AstraZeneca | 2D 3D TSV |
| 12941311 | 34 | Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines. |
Bioorg Med Chem Lett 13: 2955-60 (2003) | AstraZeneca | 2D 3D TSV |
| 12941292 | 7 | Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: the importance of being neutral. |
Bioorg Chem 31: 398-411 (2003) | Johns Hopkins University School of Medicine | 2D 3D TSV |
| 12940739 | 30 | Understanding binding affinity: a combined isothermal titration calorimetry/molecular dynamics study of the binding of a series of hydrophobically modified benzamidinium chloride inhibitors to trypsin. |
J Am Chem Soc 125: 10570-9 (2003) | University of Groningen | 2D 3D TSV |
| 12932138 | 3 | 10-Methoxydihydrofuscin, fuscinarin, and fuscin, novel antagonists of the human CCR5 receptor from Oidiodendron griseum. |
J Nat Prod 66: 1116-7 (2003) | MerLion Pharmaceuticals Pte Ltd | 2D 3D TSV |
| 12932120 | 3 | CT2108A and B: New fatty acid synthase inhibitors as antifungal agents. |
J Nat Prod 66: 1041-6 (2003) | Panlabs, Inc | 2D 3D TSV |
| 12930155 | 20 | Pyrazole derivatives as partial agonists for the nicotinic acid receptor. |
J Med Chem 46: 3945-51 (2003) | Leiden/Amsterdam Center for Drug Research | 2D 3D TSV |
| 12930154 | 6 | A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. |
J Med Chem 46: 3938-44 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12930153 | 128 | Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors. |
J Med Chem 46: 3930-7 (2003) | Virginia Commonwealth University | 2D 3D TSV |
| 12930151 | 1 | Synthesis and biological evaluation of novel flavone-8-acetic acid derivatives as reversible inhibitors of aminopeptidase N/CD13. |
J Med Chem 46: 3900-13 (2003) | Institut Curie | 2D 3D TSV |
| 12930150 | 155 | N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands. |
J Med Chem 46: 3883-99 (2003) | Johann Wolfgang Goethe-Universität | 2D 3D TSV |
| 12930149 | 37 | Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases. |
J Med Chem 46: 3877-82 (2003) | Institute of Research | 2D 3D TSV |
| 12930148 | 41 | Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone. |
J Med Chem 46: 3865-76 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12930147 | 96 | Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. |
J Med Chem 46: 3853-64 (2003) | Universit£ degli Studi di Siena | 2D 3D TSV |
| 12930146 | 170 | Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors. |
J Med Chem 46: 3840-52 (2003) | Institut de Recherches Servier | 2D 3D TSV |
| 12930145 | 77 | Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors. |
J Med Chem 46: 3822-39 (2003) | Universit£ di Siena | 2D 3D TSV |
| 12930144 | 28 | 3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase. |
J Med Chem 46: 3811-21 (2003) | Ghent University | 2D 3D TSV |
| 12930139 | 22 | Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition. |
J Med Chem 46: 3778-81 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12930138 | 1 | N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor. |
J Med Chem 46: 3775-7 (2003) | Ewha Womans University | 2D 3D TSV |
| 12930137 | 2 | Structure-based design of a macrocyclic inhibitor for peptide deformylase. |
J Med Chem 46: 3771-4 (2003) | The Ohio State University | 2D 3D TSV |
| 12924948 | 1 | Characterization of the role of polar amino acid residues within predicted transmembrane helix 17 in determining the substrate specificity of multidrug resistance protein 3. |
Biochemistry 42: 9989-10000 (2003) | Queen's University | 2D 3D TSV |
| 12921854 | 130 | Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. |
Eur J Pharmacol 474: 137-40 (2003) | Harvard University | 2D 3D TSV |
| 12904082 | 20 | New potential uroselective NO-donor alpha1-antagonists. |
J Med Chem 46: 3762-5 (2003) | Università degli Studi di Torino | 2D 3D TSV |
| 12904080 | 5 | Bispyridinium cyclophanes: novel templates for human choline kinase inhibitors. |
J Med Chem 46: 3754-7 (2003) | Universidad de Granada | 2D 3D TSV |
| 12904077 | 75 | Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. |
J Med Chem 46: 3728-33 (2003) | University of Arizona | 2D 3D TSV |
| 12904076 | 158 | A novel class of nonpeptidic biaryl inhibitors of human cathepsin K. |
J Med Chem 46: 3709-27 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12904075 | 32 | A comparison of phosphonothioic acids with phosphonic acids as phosphatase inhibitors. |
J Med Chem 46: 3703-8 (2003) | Utah State University | 2D 3D TSV |
| 12904069 | 24 | Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens. |
J Med Chem 46: 3655-61 (2003) | Procter & Gamble Pharmaceuticals | 2D 3D TSV |
| 12904068 | 5 | Structure-based design and synthesis of novel potent Na+,K+ -ATPase inhibitors derived from a 5alpha,14alpha-androstane scaffold as positive inotropic compounds. |
J Med Chem 46: 3644-54 (2003) | Prassis Istituto di Ricerche Sigma-Tau | 2D 3D TSV |
| 12904065 | 30 | Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide. |
J Med Chem 46: 3612-22 (2003) | LG Life Sciences Ltd | 2D 3D TSV |
| 12904063 | 69 | Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators. |
J Med Chem 46: 3581-99 (2003) | Kyorin Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12904061 | 17 | Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands. |
J Med Chem 46: 3568-71 (2003) | Universit£ degli Studi di Siena | 2D 3D TSV |
| 12904059 | 10 | Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. |
J Med Chem 46: 3563-4 (2003) | Institut f£r Molekularbiologie und Biophysik | 2D 3D TSV |
| 12904058 | 2 | Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2. |
J Med Chem 46: 3559-62 (2003) | National Institutes of Health | 2D 3D TSV |
| 12897767 | 18 | Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity. |
Nat Struct Biol 10: 764-9 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12893846 | 3 | A natural product ligand of the oxysterol receptor, liver X receptor. |
J Pharmacol Exp Ther 307: 291-6 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12892559 | 2 | Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition. |
Biochem J 375: 255-62 (2003) | University of Dundee | 2D 3D TSV |
| 12887776 | 4 | [BRCA1 protein expression in sporadic breast and its clinical significance]. |
Zhonghua Wai Ke Za Zhi 41: 186-8 (2003) | Anhui Medical University | 2D 3D TSV |
| 12887410 | 15 | Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist. |
Eur J Neurosci 18: 290-5 (2003) | University of Innsbruck | 2D 3D TSV |
| 12880321 | 2 | Acetophenone derivatives from Acronychia pedunculata. |
J Nat Prod 66: 990-3 (2003) | National Cheng Kung University | 2D 3D TSV |
| 12880315 | 3 | Antiparasitic alkaloids from Psychotria klugii. |
J Nat Prod 66: 962-7 (2003) | University of Mississippi | 2D 3D TSV |
| 12880313 | 33 | Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action. |
J Nat Prod 66: 954-7 (2003) | Universidad de Chile | 2D 3D TSV |
| 12877594 | 14 | Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety. |
J Med Chem 46: 3555-8 (2003) | Università di Pisa | 2D 3D TSV |
| 12877591 | 36 | Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands. |
J Med Chem 46: 3526-35 (2003) | Purdue University | 2D 3D TSV |
| 12877590 | 28 | A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. |
J Med Chem 46: 3514-25 (2003) | Pfizer Inc | 2D 3D TSV |
| 12877589 | 2 | Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist. |
J Med Chem 46: 3508-13 (2003) | Novartis Pharma AG | 2D 3D TSV |
| 12877587 | 6 | Development of a water-soluble matrix metalloproteinase inhibitor as an intra-arterial infusion drug for prevention of restenosis after angioplasty. |
J Med Chem 46: 3497-501 (2003) | National Cardiovascular Center Research Institute | 2D 3D TSV |
| 12877586 | 40 | A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain. |
J Med Chem 46: 3483-96 (2003) | Organix Inc | 2D 3D TSV |
| 12877584 | 182 | Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. |
J Med Chem 46: 3463-75 (2003) | Domp&egrove; pha.r.ma s.p.a. | 2D 3D TSV |
| 12877583 | 13 | Design and synthesis of dihydrofolate reductase inhibitors encompassing a bridging ester group. Evaluation in a mouse colitis model. |
J Med Chem 46: 3455-62 (2003) | Uppsala University | 2D 3D TSV |
| 12877582 | 3 | Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis. |
J Med Chem 46: 3452-4 (2003) | Johns Hopkins University School of Medicine | 2D 3D TSV |
| 12877579 | 6 | Identification of"latent hits" in compound screening collections. |
J Med Chem 46: 3441-4 (2003) | Organon Laboratories Ltd | 2D 3D TSV |
| 12877578 | 33 | Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands. |
J Med Chem 46: 3437-40 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12873518 | 81 | Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates. |
Bioorg Med Chem Lett 13: 2799-803 (2003) | Wyeth Research | 2D 3D TSV |
| 12873517 | 90 | 5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents. |
Bioorg Med Chem Lett 13: 2795-8 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12873514 | 56 | Design and synthesis of potent and selective macrocyclic thrombin inhibitors. |
Bioorg Med Chem Lett 13: 2781-4 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12873513 | 8 | Novel 3-O-acyl mesquitol analogues as free-radical scavengers and enzyme inhibitors: synthesis, biological evaluation and structure-activity relationship. |
Bioorg Med Chem Lett 13: 2777-80 (2003) | Institute of Chemical Technology | 2D 3D TSV |
| 12873512 | 68 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. |
Bioorg Med Chem Lett 13: 2773-5 (2003) | Gedeon Richter Ltd | 2D 3D TSV |
| 12873509 | 4 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one? |
Bioorg Med Chem Lett 13: 2759-63 (2003) | Università degli Studi di Firenze | 2D 3D TSV |
| 12873506 | 8 | Novel, potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures. |
Bioorg Med Chem Lett 13: 2745-8 (2003) | MRL Rome | 2D 3D TSV |
| 12873505 | 20 | Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors. |
Bioorg Med Chem Lett 13: 2741-4 (2003) | Hokkaido Collaboration Center | 2D 3D TSV |
| 12873504 | 36 | Structure--activity relationships of azasugar-based MMP/ADAM inhibitors. |
Bioorg Med Chem Lett 13: 2737-40 (2003) | Hokkaido Collaboration Center | 2D 3D TSV |
| 12873501 | 110 | Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants. |
Bioorg Med Chem Lett 13: 2719-25 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12873500 | 37 | Structure--activity relationships of the peptide deformylase inhibitor BB-3497: modification of the P2' and P3' side chains. |
Bioorg Med Chem Lett 13: 2715-8 (2003) | British Biotech Pharmaceuticals Limited | 2D 3D TSV |
| 12873499 | 25 | Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the methylene spacer and the P1' side chain. |
Bioorg Med Chem Lett 13: 2709-13 (2003) | British Biotech Pharmaceuticals Limited | 2D 3D TSV |
| 12873495 | 2 | Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lung. |
Bioorg Med Chem Lett 13: 2687-92 (2003) | University of Mainz | 2D 3D TSV |
| 12873488 | 11 | Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors. |
Bioorg Med Chem Lett 13: 2659-62 (2003) | Universit£ de Lille 2 | 2D 3D TSV |
| 12873487 | 5 | Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor. |
Bioorg Med Chem Lett 13: 2655-8 (2003) | The University of Tokyo | 2D 3D TSV |
| 12873485 | 150 | Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2). |
Bioorg Med Chem Lett 13: 2647-50 (2003) | University of Cincinnati | 2D 3D TSV |
| 12873480 | 30 | Hit-to-lead studies: the discovery of potent, orally bioavailable triazolethiol CXCR2 receptor antagonists. |
Bioorg Med Chem Lett 13: 2625-8 (2003) | AstraZeneca R&D Charnwood | 2D 3D TSV |
| 12871036 | 2 | GABA(C) receptors as drug targets. |
Curr Drug Targets CNS Neurol Disord 2: 260-8 (2003) | University of Sydney | 2D 3D TSV |
| 12857114 | 102 | High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II. |
J Comb Chem 5: 456-64 (2003) | Uppsala University | 2D 3D TSV |
| 12852973 | 63 | 2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis. |
Bioorg Med Chem Lett 13: 2591-4 (2003) | Wyeth Research | 2D 3D TSV |
| 12852972 | 79 | Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors. |
Bioorg Med Chem Lett 13: 2587-90 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12852971 | 8 | Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide. |
Bioorg Med Chem Lett 13: 2583-6 (2003) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
| 12852970 | 28 | Tripeptide inhibitors of Yersinia protein-tyrosine phosphatase. |
Bioorg Med Chem Lett 13: 2577-81 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12852969 | 13 | The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains. |
Bioorg Med Chem Lett 13: 2573-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12852968 | 17 | HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent. |
Bioorg Med Chem Lett 13: 2569-72 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12852967 | 15 | Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor. |
Bioorg Med Chem Lett 13: 2565-8 (2003) | Virginia Commonwealth University | 2D 3D TSV |
| 12852966 | 23 | Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors. |
Bioorg Med Chem Lett 13: 2561-3 (2003) | Inha University | 2D 3D TSV |
| 12852960 | 48 | Effect of structural modification on the inhibitory selectivity of rutaecarpine derivatives on human CYP1A1, CYP1A2, and CYP1B1. |
Bioorg Med Chem Lett 13: 2535-8 (2003) | National Research Institute of Chinese Medicine | 2D 3D TSV |
| 12852955 | 25 | Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones. |
Bioorg Med Chem Lett 13: 2513-8 (2003) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12852954 | 22 | 3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators. |
Bioorg Med Chem Lett 13: 2509-12 (2003) | University of California | 2D 3D TSV |
| 12852951 | 21 | 2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists. |
Bioorg Med Chem Lett 13: 2497-500 (2003) | Neurogen Corporation | 2D 3D TSV |
| 12852950 | 36 | High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate. |
Bioorg Med Chem Lett 13: 2493-6 (2003) | McMaster University | 2D 3D TSV |
| 12852948 | 10 | Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR. |
Bioorg Med Chem Lett 13: 2485-8 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12852947 | 36 | Development of 3D-QSAR models in cyclic ureidobenzenesulfonamides: human beta3-adrenergic receptor agonist. |
Bioorg Med Chem Lett 13: 2481-4 (2003) | Central Drug Research Institute | 2D 3D TSV |
| 12852946 | 69 | Comparative molecular field analysis (CoMFA) of phthalazine derivatives as phosphodiesterase IV inhibitors. |
Bioorg Med Chem Lett 13: 2473-9 (2003) | National Institute of Pharmaceutical Education and Research | 2D 3D TSV |
| 12852944 | 26 | 3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors. |
Bioorg Med Chem Lett 13: 2465-8 (2003) | Hoffmann-La Roche Inc | 2D 3D TSV |
| 12852938 | 7 | Effect of catechol derivatives on cell growth and lipoxygenase activity. |
Bioorg Med Chem Lett 13: 2435-9 (2003) | Aston University | 2D 3D TSV |
| 12852771 | 26 | Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase. |
J Med Chem 46: 3412-23 (2003) | Industrial Research Limited | 2D 3D TSV |
| 12852770 | 28 | Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors. |
J Med Chem 46: 3403-11 (2003) | Washington University | 2D 3D TSV |
| 12852768 | 32 | Novel benzylidene-9(10H)-anthracenones as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
J Med Chem 46: 3382-94 (2003) | Westphalian Wilhelms-University | 2D 3D TSV |
| 12852767 | 51 | Tethered dimers as NAD synthetase inhibitors with antibacterial activity. |
J Med Chem 46: 3371-81 (2003) | University of Alabama at Birmingham | 2D 3D TSV |
| 12852766 | 22 | Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors. |
J Med Chem 46: 3354-70 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12852764 | 20 | Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors. |
J Med Chem 46: 3333-41 (2003) | Novo Nordisk A/S | 2D 3D TSV |
| 12852763 | 20 | Computer-aided selection of potential antihypertensive compounds with dual mechanism of action. |
J Med Chem 46: 3326-32 (2003) | Institute of Biomedical Chemistry of Russian Academy of Medical Sciences | 2D 3D TSV |
| 12852762 | 10 | A computational model of binding thermodynamics: the design of cyclin-dependent kinase 2 inhibitors. |
J Med Chem 46: 3314-25 (2003) | University of California | 2D 3D TSV |
| 12852759 | 2 | A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude. |
J Med Chem 46: 3292-9 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12852756 | 5 | Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs. |
J Med Chem 46: 3257-74 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12852755 | 27 | l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance. |
J Med Chem 46: 3245-56 (2003) | The University of Georgia | 2D 3D TSV |
| 12852754 | 143 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
J Med Chem 46: 3230-44 (2003) | Eberhard-Karls-University T£bingen | 2D 3D TSV |
| 12852753 | 17 | Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'. |
J Med Chem 46: 3221-9 (2003) | National Hellenic Research Foundation | 2D 3D TSV |
| 12852751 | 34 | Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia. |
J Med Chem 46: 3201-9 (2003) | Kobe Gakuin University | 2D 3D TSV |
| 12852750 | 2 | (S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine. |
J Med Chem 46: 3197-200 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12852749 | 11 | First dual aromatase-steroid sulfatase inhibitors. |
J Med Chem 46: 3193-6 (2003) | University of Bath | 2D 3D TSV |
| 12852748 | 4 | Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine. |
J Med Chem 46: 3189-92 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12842269 | 16 | Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors. |
J Chem Neuroanat 25: 233-47 (2003) | University of Michigan | 2D 3D TSV |
| 12834274 | 8 | Asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine: preparation, resolution and biological activities toward insects and their nerve preparations. |
Biosci Biotechnol Biochem 67: 980-8 (2003) | Gifu University | 2D 3D TSV |
| 12828470 | 5 | Pochonins A-F, new antiviral and antiparasitic resorcylic acid lactones from Pochonia chlamydosporia var. catenulata. |
J Nat Prod 66: 829-37 (2003) | Bayer HealthCare | 2D 3D TSV |
| 12828454 | 8 | New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana. |
J Nat Prod 66: 739-42 (2003) | University of Karachi | 2D 3D TSV |
| 12825957 | 60 | Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge. |
J Med Chem 46: 3174-7 (2003) | University of Bath | 2D 3D TSV |
| 12825954 | 68 | A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine. |
J Med Chem 46: 3162-5 (2003) | Osaka University | 2D 3D TSV |
| 12825953 | 12 | Structural determinants of selective thyromimetics. |
J Med Chem 46: 3152-61 (2003) | University of California | 2D 3D TSV |
| 12825952 | 31 | Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries. |
J Med Chem 46: 3138-51 (2003) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12825951 | 54 | Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. |
J Med Chem 46: 3127-37 (2003) | Research Triangle Institute | 2D 3D TSV |
| 12825950 | 43 | N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor. |
J Med Chem 46: 3116-26 (2003) | Seoul National University | 2D 3D TSV |
| 12825948 | 13 | Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids. |
J Med Chem 46: 3102-8 (2003) | Università degli Studi di Milano | 2D 3D TSV |
| 12825944 | 184 | Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides. |
J Med Chem 46: 3060-71 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12825939 | 7 | Histamine-releasing activity and binding to the FcepsilonRI alpha human mast cell receptor subunit of mast cell degranulating peptide analogues with alanine substitutions. |
J Med Chem 46: 3008-12 (2003) | Mount Sinai School of Medicine | 2D 3D TSV |
| 12825937 | 63 | Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. |
J Med Chem 46: 2973-84 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12825935 | 54 | Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands. |
J Med Chem 46: 2945-57 (2003) | Novartis Pharmaceuticals | 2D 3D TSV |
| 12825934 | 55 | A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents. |
J Med Chem 46: 2932-44 (2003) | University of Illinois at Urbana-Champaign | 2D 3D TSV |
| 12825933 | 17 | Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold. |
J Med Chem 46: 2917-31 (2003) | Institut für Molekulare Physiologie | 2D 3D TSV |
| 12825932 | 61 | Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter. |
J Med Chem 46: 2908-16 (2003) | National Institute on Drug Abuse | 2D 3D TSV |
| 12825930 | 16 | New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes. |
J Med Chem 46: 2877-94 (2003) | Universit£ di Catania | 2D 3D TSV |
| 12825927 | 84 | Docking and database screening reveal new classes of Plasmodium falciparum dihydrofolate reductase inhibitors. |
J Med Chem 46: 2834-45 (2003) | Università di Modena e Reggio Emilia | 2D 3D TSV |
| 12825924 | 8 | Dihydrofolate reductase mutant with exceptional resistance to methotrexate but not to trimetrexate. |
J Med Chem 46: 2816-8 (2003) | University of Minnesota | 2D 3D TSV |
| 12825922 | 207 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
J Med Chem 46: 2795-812 (2003) | Virginia Commonwealth University | 2D 3D TSV |
| 12824047 | 99 | Novel IKK inhibitors: beta-carbolines. |
Bioorg Med Chem Lett 13: 2419-22 (2003) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12824045 | 3 | Identification of oxidation product of arbutin in mushroom tyrosinase assay system. |
Bioorg Med Chem Lett 13: 2409-12 (2003) | University of California | 2D 3D TSV |
| 12824044 | 41 | 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. |
Bioorg Med Chem Lett 13: 2405-8 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12824043 | 40 | Constrained phytoestrogens and analogues as ERbeta selective ligands. |
Bioorg Med Chem Lett 13: 2399-403 (2003) | Wyeth Research | 2D 3D TSV |
| 12824042 | 64 | Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2. |
Bioorg Med Chem Lett 13: 2393-7 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12824041 | 14 | Synthesis and structure-activity relationships of open D-Ring galanthamine analogues. |
Bioorg Med Chem Lett 13: 2389-91 (2003) | CNRS | 2D 3D TSV |
| 12824040 | 5 | Synthesis and inhibitory activity of ubiquinone-acetogenin hybrid inhibitor with bovine mitochondrial complex I. |
Bioorg Med Chem Lett 13: 2385-8 (2003) | Kyoto University | 2D 3D TSV |
| 12824039 | 56 | Novel inhibitors of procollagen C-proteinase. Part 2: glutamic acid hydroxamates. |
Bioorg Med Chem Lett 13: 2381-4 (2003) | CombiChem Inc. | 2D 3D TSV |
| 12824037 | 15 | Synthesis and biological testing of non-fluorinated analogues of levofloxacin. |
Bioorg Med Chem Lett 13: 2373-5 (2003) | Procter & Gamble Pharmaceuticals | 2D 3D TSV |
| 12824036 | 77 | 2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists. |
Bioorg Med Chem Lett 13: 2369-72 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12824035 | 39 | Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors. |
Bioorg Med Chem Lett 13: 2363-7 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12824033 | 30 | Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics. |
Bioorg Med Chem Lett 13: 2355-8 (2003) | LEAD GENE CO., LTD | 2D 3D TSV |
| 12824031 | 26 | Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors. |
Bioorg Med Chem Lett 13: 2347-50 (2003) | Tanabe Seiyaku Co., Ltd | 2D 3D TSV |
| 12824030 | 67 | 1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors. |
Bioorg Med Chem Lett 13: 2341-5 (2003) | Tanabe Seiyaku Co., Ltd | 2D 3D TSV |
| 12824029 | 21 | Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2). |
Bioorg Med Chem Lett 13: 2337-40 (2003) | Amgen Inc | 2D 3D TSV |
| 12824028 | 75 | Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3. |
Bioorg Med Chem Lett 13: 2331-6 (2003) | Pfizer Inc | 2D 3D TSV |
| 12824026 | 14 | Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. |
Bioorg Med Chem Lett 13: 2319-25 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12824023 | 6 | An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist. |
Bioorg Med Chem Lett 13: 2307-10 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12824021 | 39 | Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents. |
Bioorg Med Chem Lett 13: 2297-302 (2003) | Boehringer Ingelheim Pharma KG | 2D 3D TSV |
| 12824020 | 31 | Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives. |
Bioorg Med Chem Lett 13: 2291-5 (2003) | Boehringer Ingelheim Pharma KG | 2D 3D TSV |
| 12824018 | 6 | Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. |
Bioorg Med Chem Lett 13: 2281-4 (2003) | University of Sydney | 2D 3D TSV |
| 12824014 | 284 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
Bioorg Med Chem Lett 13: 2261-7 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12816539 | 9 | Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). |
Biochem J 374: 639-46 (2003) | University of Padova | 2D 3D TSV |
| 12816482 | 38 | Complexation and chiral recognition thermodynamics of gamma-cyclodextrin with N-acetyl- and N-carbobenzyloxy-dipeptides possessing two aromatic rings. |
J Org Chem 68: 5228-35 (2003) | Japan Science and Technology Agency | 2D 3D TSV |
| 12815170 | 15 | [125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding. |
Mol Pharmacol 64: 143-53 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12801241 | 4 | Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain. |
J Med Chem 46: 2790-3 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12801240 | 105 | 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. |
J Med Chem 46: 2774-89 (2003) | Novartis Institute for BioMedical Research | 2D 3D TSV |
| 12801237 | 19 | Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. |
J Med Chem 46: 2740-54 (2003) | University of Pittsburgh | 2D 3D TSV |
| 12801236 | 34 | Synthesis of substituted 6-anilinouracils and their inhibition of DNA polymerase IIIC and Gram-positive bacterial growth. |
J Med Chem 46: 2731-9 (2003) | GLSynthesis Inc. | 2D 3D TSV |
| 12801235 | 5 | Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents. |
J Med Chem 46: 2716-30 (2003) | University of Vermont | 2D 3D TSV |
| 12801232 | 71 | Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes. |
J Med Chem 46: 2683-96 (2003) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
| 12801228 | 18 | The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity. |
J Med Chem 46: 2641-55 (2003) | Wroclaw University of Technology | 2D 3D TSV |
| 12801227 | 87 | Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae. |
J Med Chem 46: 2631-40 (2003) | Chinese Academy of Sciences | 2D 3D TSV |
| 12801226 | 6 | Utilization of a beta-aminophosphotyrosyl mimetic in the design and synthesis of macrocyclic Grb2 SH2 domain-binding peptides. |
J Med Chem 46: 2621-30 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12801225 | 16 | Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors. |
J Med Chem 46: 2606-20 (2003) | UMR C8076 (CNRS) | 2D 3D TSV |
| 12801224 | 16 | Characterization of a series of 3-amino-2-phenylpropene derivatives as novel bovine chromaffin vesicular monoamine transporter inhibitors. |
J Med Chem 46: 2599-605 (2003) | Wichita State University | 2D 3D TSV |
| 12801223 | 71 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
J Med Chem 46: 2589-98 (2003) | NIDA-IRP | 2D 3D TSV |
| 12801222 | 76 | Inhibition of Cdc25 phosphatases by indolyldihydroxyquinones. |
J Med Chem 46: 2580-8 (2003) | Duke University | 2D 3D TSV |
| 12801221 | 16 | QSAR and proteo-chemometric analysis of the interaction of a series of organic compounds with melanocortin receptor subtypes. |
J Med Chem 46: 2572-9 (2003) | Uppsala University | 2D 3D TSV |
| 12801220 | 16 | Spirocyclopropyl beta-lactams as mechanism-based inhibitors of serine beta-lactamases. Synthesis by rhodium-catalyzed cyclopropanation of 6-diazopenicillanate sulfone. |
J Med Chem 46: 2569-71 (2003) | Wyeth Research | 2D 3D TSV |
| 12798341 | 1 | Borrelidin induces the transcription of amino acid biosynthetic enzymes via a GCN4-dependent pathway. |
Bioorg Med Chem Lett 13: 2235-7 (2003) | Boston University | 2D 3D TSV |
| 12798340 | 66 | Discovery of a potent and selective series of pyrazole bacterial methionyl-tRNA synthetase inhibitors. |
Bioorg Med Chem Lett 13: 2231-4 (2003) | Cubist Pharmaceutical Inc. | 2D 3D TSV |
| 12798337 | 6 | Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents. |
Bioorg Med Chem Lett 13: 2217-22 (2003) | Indiana University School of Medicine | 2D 3D TSV |
| 12798336 | 21 | 4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor. |
Bioorg Med Chem Lett 13: 2211-5 (2003) | Pfizer Inc | 2D 3D TSV |
| 12798335 | 22 | 6-Alkyl, alkoxy, or alkylthio-substituted 3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective cyclooxygenase-2 inhibitors. |
Bioorg Med Chem Lett 13: 2205-9 (2003) | University of Alberta | 2D 3D TSV |
| 12798334 | 18 | High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus. |
Bioorg Med Chem Lett 13: 2199-203 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12798333 | 56 | Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists. |
Bioorg Med Chem Lett 13: 2195-8 (2003) | Wyeth Research | 2D 3D TSV |
| 12798332 | 35 | Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists. |
Bioorg Med Chem Lett 13: 2191-4 (2003) | Wyeth Research | 2D 3D TSV |
| 12798330 | 63 | N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists. |
Bioorg Med Chem Lett 13: 2179-83 (2003) | National Institute on Drug Abuse-Intramural Research Program | 2D 3D TSV |
| 12798329 | 18 | Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics. |
Bioorg Med Chem Lett 13: 2173-7 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12798328 | 87 | Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2. |
Bioorg Med Chem Lett 13: 2167-72 (2003) | Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories | 2D 3D TSV |
| 12798324 | 36 | Bivalent biogenic amine reuptake inhibitors. |
Bioorg Med Chem Lett 13: 2151-4 (2003) | Human BioMolecular Research Institute | 2D 3D TSV |
| 12798323 | 72 | Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117. |
Bioorg Med Chem Lett 13: 2145-9 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12798321 | 26 | Nicotinyl aspartyl ketones as inhibitors of caspase-3. |
Bioorg Med Chem Lett 13: 2137-40 (2003) | Merck Frosst Canada & Co. | 2D 3D TSV |
| 12798320 | 64 | A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines. |
Bioorg Med Chem Lett 13: 2131-5 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12798316 | 25 | 2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships. |
Bioorg Med Chem Lett 13: 2113-8 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12798313 | 19 | Novel inhibitors of procollagen C-terminal proteinase. Part 1: diamino Acid hydroxamates. |
Bioorg Med Chem Lett 13: 2101-4 (2003) | CombiChem Inc. | 2D 3D TSV |
| 12798312 | 22 | Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. |
Bioorg Med Chem Lett 13: 2097-100 (2003) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12784105 | 53 | Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. |
Neuropsychopharmacology 28: 1400-11 (2003) | Case Western Reserve University | 2D 3D TSV |
| 12781199 | 64 | Urea small molecule agonists on mouse melanocortin receptors. |
Bioorg Med Chem Lett 13: 2079-82 (2003) | University of Florida | 2D 3D TSV |
| 12781198 | 108 | Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. |
Bioorg Med Chem Lett 13: 2075-8 (2003) | Ligand Pharmaceuticals | 2D 3D TSV |
| 12781197 | 59 | Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators. |
Bioorg Med Chem Lett 13: 2071-4 (2003) | Ligand Pharmaceuticals | 2D 3D TSV |
| 12781195 | 49 | Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety. |
Bioorg Med Chem Lett 13: 2059-63 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12781194 | 1 | 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
Bioorg Med Chem Lett 13: 2055-8 (2003) | Pfizer Inc | 2D 3D TSV |
| 12781193 | 36 | 3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity. |
Bioorg Med Chem Lett 13: 2051-3 (2003) | Ligand Pharmaceuticals | 2D 3D TSV |
| 12781191 | 11 | Inhibition of mandelate racemase by alpha-fluorobenzylphosphonates. |
Bioorg Med Chem Lett 13: 2041-4 (2003) | Dalhousie University | 2D 3D TSV |
| 12781190 | 113 | Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bioorg Med Chem Lett 13: 2035-40 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12781189 | 6 | D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety. |
Bioorg Med Chem Lett 13: 2029-33 (2003) | BASF AG | 2D 3D TSV |
| 12781187 | 15 | Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bioorg Med Chem Lett 13: 2021-4 (2003) | Organon K.K. | 2D 3D TSV |
| 12781183 | 12 | The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles. |
Bioorg Med Chem Lett 13: 2003-7 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12781182 | 81 | Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents. |
Bioorg Med Chem Lett 13: 1997-2001 (2003) | Novartis Pharma AG | 2D 3D TSV |
| 12781181 | 8 | The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V). |
Bioorg Med Chem Lett 13: 1993-6 (2003) | The University of Georgia | 2D 3D TSV |
| 12781180 | 24 | Structure-activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles, core-modified analogues and amide isosteres. |
Bioorg Med Chem Lett 13: 1989-92 (2003) | Pfizer Inc | 2D 3D TSV |
| 12781179 | 4 | Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside. |
Bioorg Med Chem Lett 13: 1985-8 (2003) | Georgia Institute of Technology | 2D 3D TSV |
| 12781178 | 33 | Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors. |
Bioorg Med Chem Lett 13: 1981-4 (2003) | Schering AG | 2D 3D TSV |
| 12781177 | 7 | Hemisynthesis and preliminary evaluation of novel endocannabinoid analogues. |
Bioorg Med Chem Lett 13: 1977-80 (2003) | UMR CNRS 5074 | 2D 3D TSV |
| 12781174 | 18 | Sphingomyelin analogues as inhibitors of sphingomyelinase. |
Bioorg Med Chem Lett 13: 1963-6 (2003) | Taisho Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12781173 | 28 | Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine. |
Bioorg Med Chem Lett 13: 1959-61 (2003) | The Schering Plough Research Institute | 2D 3D TSV |
| 12773058 | 15 | Analysis of 6-(2,2-Dichloroacetamido)chrysene interaction with the hypoxanthine phosphoribosyltransferase from Trypanosoma cruzi. |
J Med Chem 46: 2548-50 (2003) | University of Connecticut | 2D 3D TSV |
| 12773056 | 21 | Synthesis and antitumor activity of novel O-carbamoylmethyloxime derivatives of radicicol. |
J Med Chem 46: 2534-41 (2003) | Pharmaceutical Research Institute | 2D 3D TSV |
| 12773053 | 2 | Design, synthesis, and evaluation of analogues of 3,3,3-trifluoro-2-hydroxy-2-phenyl-propionamide as orally available general anesthetics. |
J Med Chem 46: 2494-501 (2003) | University of Virginia | 2D 3D TSV |
| 12773052 | 14 | Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
J Med Chem 46: 2482-93 (2003) | Sapienza University of Rome | 2D 3D TSV |
| 12773050 | 26 | Discovery and structure-activity relationships of novel piperidine inhibitors of farnesyltransferase. |
J Med Chem 46: 2467-73 (2003) | Pharmaceutical Research Institute | 2D 3D TSV |
| 12773048 | 88 | Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives. |
J Med Chem 46: 2446-55 (2003) | Shionogi & Co., Ltd | 2D 3D TSV |
| 12773047 | 94 | Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives. |
J Med Chem 46: 2436-45 (2003) | Shionogi & Co., Ltd | 2D 3D TSV |
| 12773045 | 27 | Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity. |
J Med Chem 46: 2413-26 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12773044 | 18 | Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability. |
J Med Chem 46: 2404-12 (2003) | Abbott GmbH & Co. KG | 2D 3D TSV |
| 12773042 | 195 | Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. |
J Med Chem 46: 2376-96 (2003) | Wyeth Research | 2D 3D TSV |
| 12773041 | 119 | Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. |
J Med Chem 46: 2361-75 (2003) | Wyeth Research | 2D 3D TSV |
| 12773040 | 41 | Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors. |
J Med Chem 46: 2352-60 (2003) | Università degli Studi di Urbino Carlo Bo | 2D 3D TSV |
| 12773039 | 37 | Three dimensional pharmacophore modeling of human CYP17 inhibitors. Potential agents for prostate cancer therapy. |
J Med Chem 46: 2345-51 (2003) | Accelrys | 2D 3D TSV |
| 12773038 | 130 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. |
J Med Chem 46: 2334-44 (2003) | Novartis Pharma | 2D 3D TSV |
| 12773035 | 56 | Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening. |
J Med Chem 46: 2304-12 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12773033 | 17 | A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one. |
J Med Chem 46: 2283-6 (2003) | Pfizer Inc | 2D 3D TSV |
| 12773032 | 4 | 3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy. |
J Med Chem 46: 2279-82 (2003) | University of Bologna | 2D 3D TSV |
| 12773029 | 8 | Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites. |
J Med Chem 46: 2261-70 (2003) | Technische Universit£t Darmstadt | 2D 3D TSV |
| 12767917 | 30 | Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates. |
Biochem Biophys Res Commun 305: 909-14 (2003) | St. Mary's Hospital | 2D 3D TSV |
| 12762821 | 2 | Isolation and synthesis of a new bioactive ellagic acid derivative from Combretum yunnanensis. |
J Nat Prod 66: 729-31 (2003) | Teikyo University | 2D 3D TSV |
| 12762808 | 2 | New sesquiterpene quinols from a Micronesian sponge, Aka sp. |
J Nat Prod 66: 686-9 (2003) | University of Oklahoma | 2D 3D TSV |
| 12762803 | 8 | Brominated polyacetylenes from the Philippines sponge Diplastrella sp. |
J Nat Prod 66: 667-70 (2003) | University of California at San Diego | 2D 3D TSV |
| 12761343 | 23 | Developmental expression of heteromeric nicotinic receptor subtypes in chick retina. |
Mol Pharmacol 63: 1329-37 (2003) | University of Milan | 2D 3D TSV |
| 12761331 | 97 | 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. |
Mol Pharmacol 63: 1223-9 (2003) | Case Western Reserve University | 2D 3D TSV |
| 12757844 | 9 | In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand. |
Life Sci 73: 371-9 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12750432 | 19 | The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. |
J Pharmacol Exp Ther 306: 954-64 (2003) | Institut de Recherches Servier | 2D 3D TSV |
| 12749904 | 34 | Synthesis and SAR of cis-1-benzoyl-1,2,3,4-tetrahydroquinoline ligands for control of gene expression in ecdysone responsive systems. |
Bioorg Med Chem Lett 13: 1943-6 (2003) | RHeoGene | 2D 3D TSV |
| 12749903 | 69 | Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors. |
Bioorg Med Chem Lett 13: 1939-42 (2003) | SUGEN, Inc. | 2D 3D TSV |
| 12749902 | 5 | Antifungal activity of a Candida albicans GGTase I inhibitor-alanine conjugate. Inhibition of Rho1p prenylation in C. albicans. |
Bioorg Med Chem Lett 13: 1935-7 (2003) | GPC Biotech, Inc. | 2D 3D TSV |
| 12749901 | 10 | Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins. |
Bioorg Med Chem Lett 13: 1931-4 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12749900 | 29 | 6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain. |
Bioorg Med Chem Lett 13: 1927-30 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12749899 | 17 | Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. |
Bioorg Med Chem Lett 13: 1923-6 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12749898 | 11 | A novel estrogen receptor ligand template. |
Bioorg Med Chem Lett 13: 1919-22 (2003) | Bayer Corporation | 2D 3D TSV |
| 12749896 | 47 | Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues. |
Bioorg Med Chem Lett 13: 1911-4 (2003) | Rensselaer Polytechnic Institute | 2D 3D TSV |
| 12749895 | 37 | Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs). |
Bioorg Med Chem Lett 13: 1907-10 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12749894 | 48 | Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1. |
Bioorg Med Chem Lett 13: 1903-5 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12749893 | 37 | Indole amide hydroxamic acids as potent inhibitors of histone deacetylases. |
Bioorg Med Chem Lett 13: 1897-901 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12749892 | 42 | N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists. |
Bioorg Med Chem Lett 13: 1891-5 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12749891 | 37 | Potent, selective inhibitors of protein tyrosine phosphatase 1B. |
Bioorg Med Chem Lett 13: 1887-90 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12749890 | 37 | Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression. |
Bioorg Med Chem Lett 13: 1883-6 (2003) | RHeoGene | 2D 3D TSV |
| 12749889 | 2 | Design and synthesis of novel pyrrolidine-containing bradykinin antagonists. |
Bioorg Med Chem Lett 13: 1879-82 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12749888 | 63 | Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists. |
Bioorg Med Chem Lett 13: 1873-8 (2003) | Roche Bioscience | 2D 3D TSV |
| 12749886 | 7 | Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR). |
Bioorg Med Chem Lett 13: 1865-8 (2003) | Universit£ di Perugia | 2D 3D TSV |
| 12749885 | 4 | Amide analogues of TSA: synthesis, binding mode analysis and HDAC inhibition. |
Bioorg Med Chem Lett 13: 1861-4 (2003) | Vrije Universiteit Brussel | 2D 3D TSV |
| 12749884 | 126 | Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. |
Bioorg Med Chem Lett 13: 1857-9 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12747796 | 39 | Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO). |
J Med Chem 46: 2246-9 (2003) | The Danish University of Pharmaceutical Sciences | 2D 3D TSV |
| 12747794 | 124 | Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition. |
J Med Chem 46: 2227-40 (2003) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
| 12747793 | 32 | C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists. |
J Med Chem 46: 2216-26 (2003) | University of North Carolina at Chapel Hill | 2D 3D TSV |
| 12747792 | 12 | Interaction of cis-(6-benzhydrylpiperidin-3-yl)benzylamine analogues with monoamine transporters: structure-activity relationship study of structurally constrained 3,6-disubstituted piperidine analogues of (2,2-diphenylethyl)-[1-(4-fluorobenzyl)piperidin-4-ylmethyl]amine. |
J Med Chem 46: 2205-15 (2003) | Wayne State University | 2D 3D TSV |
| 12747791 | 91 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, tumor-associated isozyme IX with sulfamates including EMATE also acting as steroid sulfatase inhibitors. |
J Med Chem 46: 2197-204 (2003) | University of Montpellier | 2D 3D TSV |
| 12747790 | 171 | Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. |
J Med Chem 46: 2187-96 (2003) | University of Agricultural Sciences and Veterinary Medicine | 2D 3D TSV |
| 12747789 | 29 | Metal coordination-based inhibitors of adenylyl cyclase: novel potent P-site antagonists. |
J Med Chem 46: 2177-86 (2003) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12747788 | 41 | Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues. |
J Med Chem 46: 2169-76 (2003) | Universit£ degli Studi di Camerino | 2D 3D TSV |
| 12747787 | 106 | Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein. |
J Med Chem 46: 2152-68 (2003) | Pfizer Inc | 2D 3D TSV |
| 12747784 | 28 | Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites. |
J Med Chem 46: 2117-24 (2003) | Universit£ di Bari | 2D 3D TSV |
| 12747783 | 17 | Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties. |
J Med Chem 46: 2110-6 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12747782 | 79 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
J Med Chem 46: 2104-9 (2003) | University of California | 2D 3D TSV |
| 12747781 | 29 | Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B. |
J Med Chem 46: 2093-103 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12747780 | 56 | Binding structures and potencies of oxidosqualene cyclase inhibitors with the homologous squalene-hopene cyclase. |
J Med Chem 46: 2083-92 (2003) | Albert-Ludwigs-University of Freiburg | 2D 3D TSV |
| 12747779 | 13 | Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method. |
J Med Chem 46: 2074-82 (2003) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12747776 | 67 | 3D QSAR analyses-guided rational design of novel ligands for the (alpha4)2(beta2)3 nicotinic acetylcholine receptor. |
J Med Chem 46: 2031-48 (2003) | Institut f£r Pharmazeutische Chemie der Philipps-Universit£t Marburg | 2D 3D TSV |
| 12747775 | 56 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
J Med Chem 46: 2027-30 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12747774 | 17 | Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists. |
J Med Chem 46: 2023-6 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12747773 | 13 | Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior. |
J Med Chem 46: 2017-22 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12742021 | 191 | Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors. |
J Mol Biol 329: 93-120 (2003) | Celera | 2D 3D TSV |
| 12739951 | 91 | Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases. |
J Comb Chem 5: 336-44 (2003) | University of Anterwerp | 2D 3D TSV |
| 12739759 | 25 | Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. |
Pharm Res 20: 537-44 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12731874 | 10 | Thermodynamic characterization of the binding of nucleotides to glycyl-tRNA synthetase. |
Biochemistry 42: 5333-40 (2003) | Medical College of Ohio | 2D 3D TSV |
| 12729675 | 32 | Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches. |
Bioorg Med Chem Lett 13: 1829-35 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12729674 | 6 | Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives. |
Bioorg Med Chem Lett 13: 1825-7 (2003) | Instituto Politécnico Nacional | 2D 3D TSV |
| 12729673 | 39 | Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus. |
Bioorg Med Chem Lett 13: 1821-4 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12729670 | 49 | Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold. |
Bioorg Med Chem Lett 13: 1809-12 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12729668 | 106 | 5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists. |
Bioorg Med Chem Lett 13: 1801-4 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12729667 | 47 | Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library. |
Bioorg Med Chem Lett 13: 1795-9 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12729666 | 2 | A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp. |
Bioorg Med Chem Lett 13: 1791-4 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12729664 | 14 | Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives. |
Bioorg Med Chem Lett 13: 1783-6 (2003) | Université de Reims-Champagne-Ardenne | 2D 3D TSV |
| 12729661 | 20 | Non-imidazole heterocyclic histamine H3 receptor antagonists. |
Bioorg Med Chem Lett 13: 1767-70 (2003) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12729659 | 29 | 4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. |
Bioorg Med Chem Lett 13: 1759-62 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12729655 | 51 | Structure-activity relationship of a novel class of naphthyl amide KATP channel openers. |
Bioorg Med Chem Lett 13: 1741-4 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12729652 | 1 | Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics. |
Bioorg Med Chem Lett 13: 1729-32 (2003) | Peking University | 2D 3D TSV |
| 12729650 | 2 | Solid-phase synthesis of endothelin receptor antagonists. |
Bioorg Med Chem Lett 13: 1721-4 (2003) | BASF AG | 2D 3D TSV |
| 12729649 | 16 | Synthesis and pharmacological activity of fluorescent histamine H2 receptor antagonists related to potentidine. |
Bioorg Med Chem Lett 13: 1717-20 (2003) | Peking University | 2D 3D TSV |
| 12729646 | 24 | New fibrinolytic agents: benzothiophene derivatives as inhibitors of the t-PA-PAI-1 complex formation. |
Bioorg Med Chem Lett 13: 1705-8 (2003) | Institut de Recherches Servier | 2D 3D TSV |
| 12729643 | 31 | Discovery of novel low molecular weight inhibitors of IMPDH via virtual needle screening. |
Bioorg Med Chem Lett 13: 1691-4 (2003) | Roche Discovery Welwyn | 2D 3D TSV |
| 12729639 | 20 | 2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors. |
Bioorg Med Chem Lett 13: 1673-7 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12729633 | 3 | Inactivation of S-adenosyl-L-homocysteine hydrolase with novel 5'-thioadenosine derivatives. Antiviral effects. |
Bioorg Med Chem Lett 13: 1649-52 (2003) | UMR 6519 | 2D 3D TSV |
| 12729631 | 16 | Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors. |
Bioorg Med Chem Lett 13: 1639-43 (2003) | Dr. Reddy's Laboratories Ltd | 2D 3D TSV |
| 12729627 | 4 | Structure-activity relationship on human serum paraoxonase (PON1) using substrate analogues and inhibitors. |
Bioorg Med Chem Lett 13: 1623-6 (2003) | The University of Birmingham | 2D 3D TSV |
| 12729570 | 8 | Synthesis and tyrosinase inhibitory activity of novel N-hydroxybenzyl-N-nitrosohydroxylamines. |
Bioorg Chem 31: 129-35 (2003) | Keio University | 2D 3D TSV |
| 12725862 | 9 | Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. |
Chem Biol 10: 341-9 (2003) | University of North Carolina at Chapel Hill | 2D 3D TSV |
| 12723963 | 41 | Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents. |
J Med Chem 46: 2008-16 (2003) | Vrije Universiteit | 2D 3D TSV |
| 12723962 | 69 | Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. |
J Med Chem 46: 1997-2007 (2003) | Georgetown University Medical Center | 2D 3D TSV |
| 12723961 | 15 | Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. |
J Med Chem 46: 1989-96 (2003) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12723960 | 58 | Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure. |
J Med Chem 46: 1980-8 (2003) | Hokkaido University | 2D 3D TSV |
| 12723959 | 61 | Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives. |
J Med Chem 46: 1962-79 (2003) | Université d'Orléans | 2D 3D TSV |
| 12723956 | 22 | Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues. |
J Med Chem 46: 1940-7 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12723954 | 47 | Design of selective peptidomimetic agonists for the human orphan receptor BRS-3. |
J Med Chem 46: 1918-30 (2003) | Technische Universität München | 2D 3D TSV |
| 12723951 | 7 | Antiviral amphipathic oligo- and polyribonucleotides: analogue development and biological studies. |
J Med Chem 46: 1878-85 (2003) | University of Utah | 2D 3D TSV |
| 12723950 | 2 | 2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications. |
J Med Chem 46: 1870-7 (2003) | Deakin University | 2D 3D TSV |
| 12723949 | 9 | Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents. |
J Med Chem 46: 1858-69 (2003) | University of Pennsylvania | 2D 3D TSV |
| 12723948 | 30 | Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids. |
J Med Chem 46: 1845-57 (2003) | Ajinomoto Co. Inc | 2D 3D TSV |
| 12723947 | 10 | Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors. |
J Med Chem 46: 1831-44 (2003) | University of Pennsylvania | 2D 3D TSV |
| 12723945 | 167 | Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors. |
J Med Chem 46: 1811-23 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12723943 | 29 | Benzodiazepines as potent and selective bradykinin B1 antagonists. |
J Med Chem 46: 1803-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12723942 | 38 | Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase. |
J Med Chem 46: 1799-802 (2003) | Elan Pharmaceuticals | 2D 3D TSV |
| 12723940 | 145 | 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy. |
J Med Chem 46: 1775-94 (2003) | Research Triangle Institute | 2D 3D TSV |
| 12721338 | 61 | N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties. |
J Pharmacol Exp Ther 306: 377-86 (2003) | Pudue Pharma Discovery Research | 2D 3D TSV |
| 12720388 | 14 | Dihydropiperazine neonicotinoid compounds. Synthesis and insecticidal activity. |
J Agric Food Chem 51: 3035-42 (2003) | Dow AgroSciences | 2D 3D TSV |
| 12714592 | 8 | Identification and characterization of a novel RF-amide peptide ligand for orphan G-protein-coupled receptor SP9155. |
J Biol Chem 278: 27652-7 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12713420 | 2 | Callysponginol sulfate A, an MT1-MMP inhibitor isolated from the marine sponge Callyspongia truncata. |
J Nat Prod 66: 569-71 (2003) | The University of Tokyo | 2D 3D TSV |
| 12713414 | 2 | Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp. |
J Nat Prod 66: 551-3 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12713409 | 7 | Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria lateriflora. |
J Nat Prod 66: 535-7 (2003) | Tom's of Maine | 2D 3D TSV |
| 12704428 | 9 | Insights into antifolate resistance from malarial DHFR-TS structures. |
Nat Struct Biol 10: 257-65 (2003) | Mahidol University | 2D 3D TSV |
| 12704225 | 26 | Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram. |
J Pharmacol Exp Ther 305: 565-72 (2003) | University of Tennessee | 2D 3D TSV |
| 12700464 | 1 | Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. |
AIDS 17: 1092-4 (2003) | Tufts University School of Medicine | 2D 3D TSV |
| 12699763 | 6 | The selective inhibition of phosphatases by natural toxins: the anhydride domain of tautomycin is not a primary factor in controlling PP1/PP2A selectivity. |
Bioorg Med Chem Lett 13: 1597-600 (2003) | University of California Irvine | 2D 3D TSV |
| 12699762 | 27 | Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter. |
Bioorg Med Chem Lett 13: 1591-5 (2003) | Wayne State University | 2D 3D TSV |
| 12699761 | 85 | New scaffolds in the development of mu opioid-receptor ligands. |
Bioorg Med Chem Lett 13: 1585-9 (2003) | AstraZeneca R&D Montreal | 2D 3D TSV |
| 12699760 | 19 | 5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
Bioorg Med Chem Lett 13: 1581-4 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12699759 | 32 | 5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
Bioorg Med Chem Lett 13: 1577-80 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12699757 | 72 | Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability. |
Bioorg Med Chem Lett 13: 1571-4 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12699755 | 4 | Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam. |
Bioorg Med Chem Lett 13: 1561-4 (2003) | University of Montpellier | 2D 3D TSV |
| 12699753 | 12 | Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors. |
Bioorg Med Chem Lett 13: 1553-5 (2003) | UFR des Sciences Pharmaceutiques | 2D 3D TSV |
| 12699752 | 40 | Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists. |
Bioorg Med Chem Lett 13: 1549-52 (2003) | Sookmyung Women's University | 2D 3D TSV |
| 12699751 | 18 | 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors. |
Bioorg Med Chem Lett 13: 1543-7 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12699746 | 7 | A novel metal-chelating inhibitor of protein farnesyltransferase. |
Bioorg Med Chem Lett 13: 1523-6 (2003) | Kumamoto University | 2D 3D TSV |
| 12699745 | 49 | Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity. |
Bioorg Med Chem Lett 13: 1517-21 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12699744 | 15 | Phosphate ester serum albumin affinity tags greatly improve peptide half-life in vivo. |
Bioorg Med Chem Lett 13: 1513-5 (2003) | Genentech | 2D 3D TSV |
| 12699396 | 28 | Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. |
J Med Chem 46: 1769-72 (2003) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12699395 | 5 | Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
J Med Chem 46: 1764-8 (2003) | Kyoto University | 2D 3D TSV |
| 12699394 | 30 | Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships. |
J Med Chem 46: 1758-63 (2003) | University of Innsbruck | 2D 3D TSV |
| 12699390 | 71 | Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS. |
J Med Chem 46: 1726-36 (2003) | Harvard Medical School | 2D 3D TSV |
| 12699389 | 152 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
J Med Chem 46: 1716-25 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12699385 | 25 | Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A. |
J Med Chem 46: 1670-82 (2003) | Purdue University | 2D 3D TSV |
| 12699384 | 69 | Aromatic reduced amide bond peptidomimetics as selective inhibitors of neuronal nitric oxide synthase. |
J Med Chem 46: 1661-9 (2003) | Northwestern University | 2D 3D TSV |
| 12699382 | 4 | An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study. |
J Med Chem 46: 1636-44 (2003) | Academy of Sciences of the Czech Republic | 2D 3D TSV |
| 12699381 | 31 | Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK. |
J Med Chem 46: 1627-35 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12699376 | 20 | Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
J Med Chem 46: 1580-8 (2003) | Karo Bio AB | 2D 3D TSV |
| 12699375 | 10 | Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C). |
J Med Chem 46: 1571-9 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12697690 | 15 | Pharmacological studies of thyrotropin-releasing hormone (TRH) receptors from Xenopus laevis: is xTRHR3 a TRH receptor? |
Endocrinology 144: 1842-6 (2003) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
| 12695538 | 11 | Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5. |
Mol Pharmacol 63: 1094-103 (2003) | The Netherlands Cancer Institute | 2D 3D TSV |
| 12695537 | 25 | [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. |
Mol Pharmacol 63: 1082-93 (2003) | Johnson and Johnson Pharmaceutical Research and Development, Beerse | 2D 3D TSV |
| 12694187 | 9 | Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors. |
Eur J Biochem 270: 1746-58 (2003) | Uppsala University | 2D 3D TSV |
| 12683677 | 8 | Design, synthesis and in vitro evaluation of novel derivatives as serotonin N-acetyltransferase inhibitors. |
J Enzyme Inhib Med Chem 17: 409-14 (2002) | Université de Lille | 2D 3D TSV |
| 12682217 | 7 | SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation. |
J Pharmacol Exp Ther 306: 407-20 (2003) | Sanofi-Synthelabo Research | 2D 3D TSV |
| 12679137 | 6 | Interactions of human organic anion as well as cation transporters with indoxyl sulfate. |
Eur J Pharmacol 466: 13-20 (2003) | Nagoya University School of Medicine | 2D 3D TSV |
| 12672258 | 99 | 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. |
J Med Chem 46: 1563-6 (2003) | University of Bath | 2D 3D TSV |
| 12672255 | 18 | Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate. |
J Med Chem 46: 1538-45 (2003) | Organix Inc | 2D 3D TSV |
| 12672253 | 60 | Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds. |
J Med Chem 46: 1523-30 (2003) | Freie Universit£t Berlin | 2D 3D TSV |
| 12672252 | 104 | Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase. |
J Med Chem 46: 1512-22 (2003) | Universidad Complutense | 2D 3D TSV |
| 12672251 | 9 | 1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists. |
J Med Chem 46: 1504-11 (2003) | Universit£ degli Studi di Modena e Reggio Emilia | 2D 3D TSV |
| 12672250 | 10 | N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. |
J Med Chem 46: 1492-503 (2003) | Leiden University | 2D 3D TSV |
| 12672249 | 7 | Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity. |
J Med Chem 46: 1484-91 (2003) | Free University of Berlin | 2D 3D TSV |
| 12672248 | 50 | Kinase inhibitors: not just for kinases anymore. |
J Med Chem 46: 1478-83 (2003) | Northwestern University | 2D 3D TSV |
| 12672246 | 68 | Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine. |
J Med Chem 46: 1465-9 (2003) | NIDDK | 2D 3D TSV |
| 12672245 | 54 | Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors. |
J Med Chem 46: 1456-64 (2003) | Georgia Institute of Technology | 2D 3D TSV |
| 12672242 | 8 | Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation. |
J Med Chem 46: 1429-39 (2003) | Universit£ degli Studi di Parma | 2D 3D TSV |
| 12672241 | 37 | Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives. |
J Med Chem 46: 1419-28 (2003) | Università di Pisa | 2D 3D TSV |
| 12672240 | 18 | De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor. |
J Med Chem 46: 1408-18 (2003) | SignalGene Inc. | 2D 3D TSV |
| 12672239 | 44 | Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique. |
J Med Chem 46: 1390-407 (2003) | University of Wuerzburg | 2D 3D TSV |
| 12672238 | 3 | Mechanism of action of the diazabicyclononanone-type kappa-agonists. |
J Med Chem 46: 1383-9 (2003) | Universität Würzburg | 2D 3D TSV |
| 12672235 | 15 | (S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology. |
J Med Chem 46: 1350-8 (2003) | The Danish University of Pharmaceutical Sciences | 2D 3D TSV |
| 12672234 | 64 | Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
J Med Chem 46: 1337-49 (2003) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
| 12672232 | 28 | Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor. |
J Med Chem 46: 1318-29 (2003) | Università di Ferrara | 2D 3D TSV |
| 12672231 | 18 | Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar. |
J Med Chem 46: 1306-17 (2003) | Novo Nordisk A/S | 2D 3D TSV |
| 12672230 | 22 | Generation of ligand conformations in continuum solvent consistent with protein active site topology: application to thrombin. |
J Med Chem 46: 1293-305 (2003) | Thrombosis Research Institute | 2D 3D TSV |
| 12672227 | 22 | Identification of N,N-disubstituted phenylalanines as a novel class of inhibitors of hepatitis C NS5B polymerase. |
J Med Chem 46: 1283-5 (2003) | Shire BioChem Inc | 2D 3D TSV |
| 12672226 | 9 | A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus. |
J Med Chem 46: 1279-82 (2003) | University of Maryland | 2D 3D TSV |
| 12670229 | 8 | Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy. |
J Am Chem Soc 125: 4087-96 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12668020 | 29 | Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
Bioorg Med Chem Lett 13: 1495-8 (2003) | 3-Dimensional Pharmaceuticals Inc | 2D 3D TSV |
| 12668018 | 138 | Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors. |
Bioorg Med Chem Lett 13: 1487-90 (2003) | Wyeth-Ayerst Research | 2D 3D TSV |
| 12668017 | 17 | Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists. |
Bioorg Med Chem Lett 13: 1483-6 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12668015 | 6 | Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain. |
Bioorg Med Chem Lett 13: 1475-8 (2003) | The Ohio State University | 2D 3D TSV |
| 12668013 | 42 | Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors. |
Bioorg Med Chem Lett 13: 1463-7 (2003) | Aventis Pharma Deutschland GmbH | 2D 3D TSV |
| 12668012 | 15 | From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase. |
Bioorg Med Chem Lett 13: 1459-62 (2003) | Centre de Recherche Pierre Fabre | 2D 3D TSV |
| 12668011 | 22 | Synthesis and evaluation of a novel series of farnesyl protein transferase inhibitors as non-peptidic CAAX tetrapeptide analogues. |
Bioorg Med Chem Lett 13: 1455-8 (2003) | Centre de Recherche Pierre Fabre | 2D 3D TSV |
| 12668010 | 1 | Analogues of dealanylalahopcin are inhibitors of human HIF prolyl hydroxylases. |
Bioorg Med Chem Lett 13: 1451-4 (2003) | Oxford University | 2D 3D TSV |
| 12668009 | 36 | High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition. |
Bioorg Med Chem Lett 13: 1445-9 (2003) | Molecumetics | 2D 3D TSV |
| 12668008 | 34 | 3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors. |
Bioorg Med Chem Lett 13: 1441-4 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12668005 | 21 | Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist. |
Bioorg Med Chem Lett 13: 1429-32 (2003) | Universidad Complutense | 2D 3D TSV |
| 12668004 | 76 | Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors. |
Bioorg Med Chem Lett 13: 1425-8 (2003) | Pfizer Inc | 2D 3D TSV |
| 12668002 | 57 | Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK). |
Bioorg Med Chem Lett 13: 1415-8 (2003) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
| 12668001 | 17 | Peptoid mimics of agouti related protein. |
Bioorg Med Chem Lett 13: 1409-13 (2003) | University of California | 2D 3D TSV |
| 12668000 | 29 | 3D-QSAR studies on thieno[3,2-d]pyrimidines as phosphodiesterase IV inhibitors. |
Bioorg Med Chem Lett 13: 1403-8 (2003) | National Institute of Pharmaceutical Education and Research (NIPER) | 2D 3D TSV |
| 12662104 | 1 | Two new carbazole alkaloids from Murraya koenigii. |
J Nat Prod 66: 416-8 (2003) | Chinese Academy of Sciences | 2D 3D TSV |
| 12660315 | 17 | Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor. |
J Pharmacol Exp Ther 306: 253-61 (2003) | LCG Bioscience | 2D 3D TSV |
| 12659774 | 20 | Synthesis of potent oxindole CDK2 inhibitors. |
Bioorg Med Chem 11: 1873-81 (2003) | Hoffmann-La Roche Inc | 2D 3D TSV |
| 12657288 | 102 | Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter. |
Bioorg Med Chem Lett 13: 1385-9 (2003) | NIDDK | 2D 3D TSV |
| 12657284 | 31 | Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase. |
Bioorg Med Chem Lett 13: 1367-71 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12657283 | 37 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency. |
Bioorg Med Chem Lett 13: 1363-6 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12657282 | 13 | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
Bioorg Med Chem Lett 13: 1359-62 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12657281 | 29 | Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides. |
Bioorg Med Chem Lett 13: 1353-7 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12657279 | 25 | Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors. |
Bioorg Med Chem Lett 13: 1345-8 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12657278 | 38 | Synthesis and structure--activity relationships of aroylpyrrole alkylamide bradykinin (B2) antagonists. |
Bioorg Med Chem Lett 13: 1341-4 (2003) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12657277 | 40 | Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents. |
Bioorg Med Chem Lett 13: 1337-40 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12657276 | 2 | Inhibition of telomerase by BIBR 1532 and related analogues. |
Bioorg Med Chem Lett 13: 1333-6 (2003) | University of Texas at Dallas | 2D 3D TSV |
| 12657274 | 109 | Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. |
Bioorg Med Chem Lett 13: 1325-8 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12657272 | 47 | Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists. |
Bioorg Med Chem Lett 13: 1317-20 (2003) | Wyeth Research | 2D 3D TSV |
| 12657271 | 71 | Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists. |
Bioorg Med Chem Lett 13: 1313-6 (2003) | Wyeth Research | 2D 3D TSV |
| 12657270 | 57 | Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
Bioorg Med Chem Lett 13: 1307-11 (2003) | Roche Research Center | 2D 3D TSV |
| 12657269 | 52 | Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines. |
Bioorg Med Chem Lett 13: 1301-5 (2003) | Dainippon Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12657268 | 13 | Potent and selective aggrecanase inhibitors containing cyclic P1 substituents. |
Bioorg Med Chem Lett 13: 1297-300 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12657267 | 65 | Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor. |
Bioorg Med Chem Lett 13: 1293-6 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12657266 | 3 | [3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter. |
Bioorg Med Chem Lett 13: 1291-2 (2003) | Pfizer Inc | 2D 3D TSV |
| 12657263 | 46 | Phenylacetic acid derivatives as hPPAR agonists. |
Bioorg Med Chem Lett 13: 1277-80 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12657262 | 14 | Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3. |
Bioorg Med Chem Lett 13: 1273-6 (2003) | Bristol-Myers Squibb PRI | 2D 3D TSV |
| 12657261 | 32 | Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities. |
Bioorg Med Chem Lett 13: 1269-72 (2003) | Tohoku Pharmaceutical University | 2D 3D TSV |
| 12657259 | 2 | The inhibitory effects of squalene-derived triterpenes on protein phosphatase PP2A. |
Bioorg Med Chem Lett 13: 1261-4 (2003) | Instituto Universitario de Bio-Org£nica | 2D 3D TSV |
| 12657255 | 21 | Synthesis and pharmacological activity of fluorescent histamine H1 receptor antagonists related to mepyramine. |
Bioorg Med Chem Lett 13: 1245-8 (2003) | Peking University | 2D 3D TSV |
| 12657254 | 10 | Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand. |
Bioorg Med Chem Lett 13: 1241-4 (2003) | Utrecht University | 2D 3D TSV |
| 12657252 | 15 | Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. |
Bioorg Med Chem Lett 13: 1231-5 (2003) | Eli Lilly and Company | 2D 3D TSV |
| 12650826 | 10 | Interaction of human and rat organic anion transporter 2 with various cephalosporin antibiotics. |
Eur J Pharmacol 465: 1-7 (2003) | Kyorin University | 2D 3D TSV |
| 12649369 | 6 | Inhibition of P-glycoprotein by newer antidepressants. |
J Pharmacol Exp Ther 305: 197-204 (2003) | University of Heidelberg | 2D 3D TSV |
| 12649362 | 8 | Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine. |
J Pharmacol Exp Ther 305: 143-50 (2003) | Georgetown University | 2D 3D TSV |
| 12649361 | 779 | L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists. |
J Pharmacol Exp Ther 305: 131-42 (2003) | Case Western Reserve University | 2D 3D TSV |
| 12649353 | 15 | Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors. |
J Pharmacol Exp Ther 305: 57-69 (2003) | Bristol-Myers Squibb Pharmaceuticals Research Institute | 2D 3D TSV |
| 12649305 | 4 | Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687). |
J Pharmacol Exp Ther 305: 1037-44 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12646038 | 19 | Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist. |
J Med Chem 46: 1273-6 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12646036 | 16 | 2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels. |
J Med Chem 46: 1257-65 (2003) | Massachusetts General Hospital | 2D 3D TSV |
| 12646033 | 124 | Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists. |
J Med Chem 46: 1229-41 (2003) | Universit£ di Ferrara | 2D 3D TSV |
| 12646032 | 30 | High affinity hydroxypiperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter: stereospecific interactions in vitro and in vivo. |
J Med Chem 46: 1220-8 (2003) | Wayne State University | 2D 3D TSV |
| 12646029 | 40 | New active series of growth hormone secretagogues. |
J Med Chem 46: 1191-203 (2003) | University of Montpellier | 2D 3D TSV |
| 12646027 | 43 | Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives. |
J Med Chem 46: 1165-79 (2003) | Link£ping University | 2D 3D TSV |
| 12646026 | 60 | Use of a pharmacophore model to discover a new class of influenza endonuclease inhibitors. |
J Med Chem 46: 1153-64 (2003) | Roche Discovery Welwyn | 2D 3D TSV |
| 12646025 | 12 | Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors. |
J Med Chem 46: 1144-52 (2003) | Universidade Federal do Rio de Janeiro | 2D 3D TSV |
| 12646024 | 17 | Virtual screening for submicromolar leads of tRNA-guanine transglycosylase based on a new unexpected binding mode detected by crystal structure analysis. |
J Med Chem 46: 1133-43 (2003) | Philipps-Universität Marburg | 2D 3D TSV |
| 12646022 | 22 | Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands. |
J Med Chem 46: 1127-9 (2003) | Université de Lille 2 | 2D 3D TSV |
| 12646021 | 35 | Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. |
J Med Chem 46: 1123-6 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12646020 | 17 | Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase. |
J Med Chem 46: 1120-2 (2003) | Ontogen Corporation | 2D 3D TSV |
| 12646019 | 48 | Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. |
J Med Chem 46: 1116-9 (2003) | SUGEN, Inc. | 2D 3D TSV |
| 12646018 | 27 | Synthesis and biological evaluation of non-peptidic cyclophilin ligands. |
J Med Chem 46: 1112-5 (2003) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12646017 | 1 | Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents. |
J Med Chem 46: 1081-111 (2003) | The Feinberg School of Medicine of Northwestern University | 2D 3D TSV |
| 12643946 | 32 | Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors. |
Bioorg Med Chem Lett 13: 1215-9 (2003) | National Cancer Institute-Bethesda | 2D 3D TSV |
| 12643945 | 36 | Structure-activity relationships of some opiate glycosides. |
Bioorg Med Chem Lett 13: 1207-14 (2003) | Ultrafine UFC Ltd | 2D 3D TSV |
| 12643944 | 26 | Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives. |
Bioorg Med Chem Lett 13: 1203-6 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12643943 | 43 | Indanyl piperazines as melatonergic MT2 selective agents. |
Bioorg Med Chem Lett 13: 1199-202 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12643942 | 82 | 3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility. |
Bioorg Med Chem Lett 13: 1195-8 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12643941 | 20 | N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors. |
Bioorg Med Chem Lett 13: 1191-4 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12643939 | 81 | 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds. |
Bioorg Med Chem Lett 13: 1183-6 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12643937 | 7 | Interfacial peptide inhibitors of HIV-1 integrase activity and dimerization. |
Bioorg Med Chem Lett 13: 1175-7 (2003) | Purdue University | 2D 3D TSV |
| 12643934 | 109 | Benzamide derivatives as blockers of Kv1.3 ion channel. |
Bioorg Med Chem Lett 13: 1161-4 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12643933 | 27 | Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease. |
Bioorg Med Chem Lett 13: 1157-60 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12643930 | 95 | Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods. |
Bioorg Med Chem Lett 13: 1141-5 (2003) | AstraZeneca R&D | 2D 3D TSV |
| 12643929 | 18 | Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase. |
Bioorg Med Chem Lett 13: 1137-9 (2003) | Pfizer Inc | 2D 3D TSV |
| 12643928 | 24 | 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases. |
Bioorg Med Chem Lett 13: 1133-6 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12643927 | 164 | Discovery of a potent and selective agonist of the prostaglandin EP4 receptor. |
Bioorg Med Chem Lett 13: 1129-32 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12643924 | 7 | Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors. |
Bioorg Med Chem Lett 13: 1115-8 (2003) | Fujisawa Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12643923 | 22 | Glycine alpha-ketoamides as HCV NS3 protease inhibitors. |
Bioorg Med Chem Lett 13: 1111-4 (2003) | Pharmaceutical Research Institute | 2D 3D TSV |
| 12643919 | 50 | Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists. |
Bioorg Med Chem Lett 13: 1093-6 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12643918 | 16 | N-Alkoxysulfamide, N-hydroxysulfamide, and sulfamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases. |
Bioorg Med Chem Lett 13: 1087-92 (2003) | Seoul National University | 2D 3D TSV |
| 12643914 | 40 | Biphenyls as potent vitronectin receptor antagonists. Part 2: biphenylalanine ureas. |
Bioorg Med Chem Lett 13: 1071-4 (2003) | Bayer AG | 2D 3D TSV |
| 12643913 | 55 | The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. |
Bioorg Med Chem Lett 13: 1067-70 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12643910 | 55 | Identification of a novel series of selective 5-HT7 receptor antagonists. |
Bioorg Med Chem Lett 13: 1055-8 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12643904 | 12 | Synthesis and binding affinity of neuropeptide Y at opiate receptors. |
Bioorg Med Chem Lett 13: 1029-31 (2003) | University of North Carolina at Wilmington | 2D 3D TSV |
| 12643903 | 81 | Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors. |
Bioorg Med Chem Lett 13: 1023-8 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12643901 | 42 | N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship. |
Bioorg Med Chem Lett 13: 1015-8 (2003) | Genentech | 2D 3D TSV |
| 12643899 | 127 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides. |
Bioorg Med Chem Lett 13: 1005-9 (2003) | Universit£ degli Studi di Firenze | 2D 3D TSV |
| 12643898 | 4 | Syntheses and biological properties of cysteine-reactive epibatidine derivatives. |
Bioorg Med Chem Lett 13: 1001-4 (2003) | Universit£ Louis Pasteur Strasbourg BP 24 | 2D 3D TSV |
| 12639577 | 105 | Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics. |
Bioorg Med Chem Lett 13: 767-70 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12639576 | 37 | Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors. |
Bioorg Med Chem Lett 13: 761-5 (2003) | Johnson & Johnson Pharmaceutical Research & Development LLC | 2D 3D TSV |
| 12639574 | 21 | Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists. |
Bioorg Med Chem Lett 13: 753-6 (2003) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12639573 | 9 | 1,4-dibenzylpiperazines possess anticocaine activity. |
Bioorg Med Chem Lett 13: 749-51 (2003) | University of Maryland | 2D 3D TSV |
| 12639571 | 24 | Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors. |
Bioorg Med Chem Lett 13: 741-4 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12639570 | 1 | Functional expression and characterization of EryA, the erythritol kinase of Brucella abortus, and enzymatic synthesis of L-erythritol-4-phosphate. |
Bioorg Med Chem Lett 13: 737-9 (2003) | Brown University | 2D 3D TSV |
| 12639569 | 23 | Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors. |
Bioorg Med Chem Lett 13: 733-5 (2003) | Virginia Commonwealth University | 2D 3D TSV |
| 12639568 | 52 | Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors. |
Bioorg Med Chem Lett 13: 729-32 (2003) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12639567 | 135 | Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors. |
Bioorg Med Chem Lett 13: 723-8 (2003) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12639565 | 19 | Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase. |
Bioorg Med Chem Lett 13: 713-7 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12639564 | 23 | Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides. |
Bioorg Med Chem Lett 13: 709-12 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12639563 | 4 | Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist. |
Bioorg Med Chem Lett 13: 705-8 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12639562 | 41 | Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist. |
Bioorg Med Chem Lett 13: 701-4 (2003) | Neurogen Corporation | 2D 3D TSV |
| 12639561 | 51 | Orally efficacious NR2B-selective NMDA receptor antagonists. |
Bioorg Med Chem Lett 13: 697-700 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12639560 | 34 | Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists. |
Bioorg Med Chem Lett 13: 693-6 (2003) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
| 12639557 | 7 | Exploring new non-sugar sulfated molecules as activators of antithrombin. |
Bioorg Med Chem Lett 13: 679-83 (2003) | Virginia Commonwealth University | 2D 3D TSV |
| 12639555 | 10 | Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir. |
Bioorg Med Chem Lett 13: 669-73 (2003) | Sankyo Co., Ltd | 2D 3D TSV |
| 12639554 | 67 | Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity. |
Bioorg Med Chem Lett 13: 665-8 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12639552 | 25 | Design, synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors. |
Bioorg Med Chem Lett 13: 657-60 (2003) | Vittal Mallya Scientific Research Foundation | 2D 3D TSV |
| 12639550 | 55 | Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution. |
Bioorg Med Chem Lett 13: 649-52 (2003) | Roche Research Center | 2D 3D TSV |
| 12639549 | 2 | Inhibition of inosine monophosphate dehydrogenase (IMPDH) by 2-[2-(Z)-fluorovinyl]inosine 5'-monophosphate. |
Bioorg Med Chem Lett 13: 645-7 (2003) | The University of Georgia | 2D 3D TSV |
| 12639547 | 26 | Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. |
Bioorg Med Chem Lett 13: 637-40 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12639546 | 30 | Identification of a high-affinity phosphopeptide inhibitor of Stat3. |
Bioorg Med Chem Lett 13: 633-6 (2003) | The University of Texas at Houston | 2D 3D TSV |
| 12639545 | 37 | Synthesis of dopamine transporter selective 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes. |
Bioorg Med Chem Lett 13: 629-32 (2003) | University of New Orleans | 2D 3D TSV |
| 12639541 | 26 | Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities. |
Bioorg Med Chem Lett 13: 609-12 (2003) | Seoul National University | 2D 3D TSV |
| 12639540 | 10 | Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors. |
Bioorg Med Chem Lett 13: 605-8 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12639539 | 26 | Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor. |
Bioorg Med Chem Lett 13: 601-4 (2003) | Seoul National University | 2D 3D TSV |
| 12639538 | 90 | Pyridazinones as selective cyclooxygenase-2 inhibitors. |
Bioorg Med Chem Lett 13: 597-600 (2003) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12636153 | 6 | Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter. |
Pharm Res 20: 161-8 (2003) | The University of Kansas | 2D 3D TSV |
| 12629531 | 203 | H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. |
Neuropsychopharmacology 28: 519-26 (2003) | Case Western Reserve University | 2D 3D TSV |
| 12628671 | 98 | Synthesis and pharmacological evaluation of substituted naphth[1,2,3-de]isoquinolines (dinapsoline analogues) as D1 and D2 dopamine receptor ligands. |
Bioorg Med Chem 11: 1451-64 (2003) | Purdue University | 2D 3D TSV |
| 12626648 | 19 | Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. |
J Pharmacol Exp Ther 305: 1104-15 (2003) | University of Kansas | 2D 3D TSV |
| 12620084 | 17 | QSAR and classification of murine and human soluble epoxide hydrolase inhibition by urea-like compounds. |
J Med Chem 46: 1066-80 (2003) | The Pennsylvania State University | 2D 3D TSV |
| 12620079 | 35 | Systematic development of high affinity bis(ammonio)alkane-type allosteric enhancers of muscarinic ligand binding. |
J Med Chem 46: 1031-40 (2003) | University of W£rzburg | 2D 3D TSV |
| 12620078 | 132 | Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. |
J Med Chem 46: 1016-30 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12620072 | 3 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine. |
J Med Chem 46: 954-66 (2003) | University of Bologna | 2D 3D TSV |
| 12620070 | 24 | Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography. |
J Med Chem 46: 925-35 (2003) | Emory University | 2D 3D TSV |
| 12620069 | 42 | Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. |
J Med Chem 46: 921-4 (2003) | Georgetown University Medical Center | 2D 3D TSV |
| 12620068 | 44 | Simple, potent, and selective pyrrole inhibitors of monoamine oxidase types A and B. |
J Med Chem 46: 917-20 (2003) | Sapienza University of Rome | 2D 3D TSV |
| 12620067 | 47 | 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo. |
J Med Chem 46: 913-6 (2003) | AstraZeneca R&D Charnwood | 2D 3D TSV |
| 12620065 | 1 | Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions. |
J Med Chem 46: 883-908 (2003) | The Feinberg School of Medicine of Northwestern University | 2D 3D TSV |
| 12617932 | 10 | Modification of the N-terminus of peptidomimetic protein tyrosine phosphatase 1B (PTP1B) inhibitors: identification of analogues with cellular activity. |
Bioorg Med Chem Lett 13: 971-5 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12617929 | 114 | The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists. |
Bioorg Med Chem Lett 13: 955-9 (2003) | Actelion Pharmaceuticals Ltd | 2D 3D TSV |
| 12617928 | 68 | Bis-sulfonamides as endothelin receptor antagonists. |
Bioorg Med Chem Lett 13: 951-4 (2003) | Actelion Pharmaceuticals Ltd | 2D 3D TSV |
| 12617924 | 140 | Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists. |
Bioorg Med Chem Lett 13: 931-5 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12617923 | 3 | Acylcyclohexanedione derivatives as potential in vivo sequential inhibitors of 4-hydroxyphenylpyruvate dioxygenase and GA(20) 3beta-hydroxylase. |
Bioorg Med Chem Lett 13: 927-30 (2003) | Tunghai University | 2D 3D TSV |
| 12617920 | 41 | Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1. |
Bioorg Med Chem Lett 13: 913-8 (2003) | Kyoto 619-0216 | 2D 3D TSV |
| 12617917 | 7 | Synthesis of (+),(-)-neamine and their positional isomers as potential antibiotics. |
Bioorg Med Chem Lett 13: 901-3 (2003) | Harvard Medical School | 2D 3D TSV |
| 12617916 | 13 | Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain. |
Bioorg Med Chem Lett 13: 895-9 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12617914 | 116 | N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists. |
Bioorg Med Chem Lett 13: 885-90 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12617910 | 6 | Design and synthesis of the tumor-activated prodrug of dihydropyrimidine dehydrogenase (DPD) inhibitor, RO0094889 for combination therapy with capecitabine. |
Bioorg Med Chem Lett 13: 867-72 (2003) | Nippon Roche Research Center | 2D 3D TSV |
| 12617909 | 6 | Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II. |
Bioorg Med Chem Lett 13: 863-5 (2003) | University of Bath | 2D 3D TSV |
| 12617906 | 46 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
Bioorg Med Chem Lett 13: 851-4 (2003) | Friedrich-Alexander University | 2D 3D TSV |
| 12617904 | 46 | Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. |
Bioorg Med Chem Lett 13: 841-5 (2003) | Universit£ degli Studi di Firenze | 2D 3D TSV |
| 12617903 | 65 | Carbonic anhydrase inhibitors: inhibition of cytosolic isozymes I and II with sulfamide derivatives. |
Bioorg Med Chem Lett 13: 837-40 (2003) | Universit£ degli Studi di Firenze | 2D 3D TSV |
| 12617901 | 23 | 2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists. |
Bioorg Med Chem Lett 13: 829-32 (2003) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12617898 | 13 | Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands. |
Bioorg Med Chem Lett 13: 817-20 (2003) | Seoul National University | 2D 3D TSV |
| 12617895 | 30 | Dehydrophenylalanine derivatives as VLA-4 integrin antagonists. |
Bioorg Med Chem Lett 13: 805-8 (2003) | Celltech R&D Ltd | 2D 3D TSV |
| 12617894 | 6 | An adjustable release rate linking strategy for cytotoxin-peptide conjugates. |
Bioorg Med Chem Lett 13: 799-803 (2003) | Tulane University Health Sciences Center | 2D 3D TSV |
| 12617893 | 28 | Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors. |
Bioorg Med Chem Lett 13: 795-8 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12617892 | 43 | Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics. |
Bioorg Med Chem Lett 13: 789-94 (2003) | University of Ljubljana | 2D 3D TSV |
| 12617891 | 37 | Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors. |
Bioorg Med Chem Lett 13: 785-8 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12617890 | 9 | Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics. |
Bioorg Med Chem Lett 13: 783-4 (2003) | University of Tennessee Health Science Center | 2D 3D TSV |
| 12616631 | 18 | D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. |
Chembiochem 4: 181-5 (2003) | University of Queensland Brisbane | 2D 3D TSV |
| 12608855 | 25 | Exploring sponge-derived terpenoids for their potency and selectivity against 12-human, 15-human, and 15-soybean lipoxygenases. |
J Nat Prod 66: 230-5 (2003) | University of California Santa Cruz | 2D 3D TSV |
| 12606755 | 1 | Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. |
Mol Pharmacol 63: 489-98 (2003) | University of Arizona | 2D 3D TSV |
| 12606689 | 25 | Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons. |
J Pharmacol Exp Ther 305: 740-8 (2003) | State University of New York | 2D 3D TSV |
| 12606613 | 4 | A tertiary alcohol analog of gamma-hydroxybutyric acid as a specific gamma-hydroxybutyric acid receptor ligand. |
J Pharmacol Exp Ther 305: 675-9 (2003) | University of Maryland | 2D 3D TSV |
| 12606605 | 33 | Prolactin releasing peptide has high affinity and efficacy at neuropeptide FF2 receptors. |
J Pharmacol Exp Ther 305: 825-32 (2003) | Juvantia Pharma Ltd | 2D 3D TSV |
| 12606603 | 59 | Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
J Pharmacol Exp Ther 305: 887-96 (2003) | Abbott Laboratories | 2D 3D TSV |
| 12604693 | 1 | Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein. |
J Pharmacol Exp Ther 304: 1161-71 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12593668 | 6 | Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties. |
J Med Chem 46: 876-9 (2003) | Martin-Luther-University Halle-Wittenberg | 2D 3D TSV |
| 12593666 | 30 | Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. |
J Med Chem 46: 868-71 (2003) | Senju Pharmaceutical Co. | 2D 3D TSV |
| 12593665 | 188 | Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists. |
J Med Chem 46: 856-67 (2003) | Johannes Gutenberg-University of Mainz | 2D 3D TSV |
| 12593663 | 146 | Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines. |
J Med Chem 46: 838-49 (2003) | Rensselaer Polytechnic Institute | 2D 3D TSV |
| 12593662 | 6 | Synthesis and flow cytometric evaluation of novel 1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of nitrobenzylmercaptopurine riboside (NBMPR) designed for probing its conformation when bound to the es nucleoside transporter. |
J Med Chem 46: 831-7 (2003) | University of Tennessee Health Sciences Center | 2D 3D TSV |
| 12593661 | 34 | Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. |
J Med Chem 46: 820-30 (2003) | MethylGene Inc | 2D 3D TSV |
| 12593660 | 23 | Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist. |
J Med Chem 46: 810-9 (2003) | University of Arizona | 2D 3D TSV |
| 12593657 | 66 | Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives. |
J Med Chem 46: 768-81 (2003) | Università di Genova | 2D 3D TSV |
| 12593654 | 48 | Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes. |
J Med Chem 46: 734-46 (2003) | Uppsala University | 2D 3D TSV |
| 12593652 | 50 | Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. |
J Med Chem 46: 716-26 (2003) | University of Innsbruck | 2D 3D TSV |
| 12593651 | 107 | Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity. |
J Med Chem 46: 702-15 (2003) | Dainippon Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12593650 | 11 | Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor. |
J Med Chem 46: 691-701 (2003) | Sumitomo Pharmaceuticals Co., Ltd | 2D 3D TSV |
| 12593649 | 15 | Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket. |
J Med Chem 46: 685-90 (2003) | Aventis Pharma | 2D 3D TSV |
| 12593648 | 53 | Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand. |
J Med Chem 46: 681-4 (2003) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12593647 | 49 | 2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists. |
J Med Chem 46: 677-80 (2003) | Harvard University | 2D 3D TSV |
| 12593646 | 13 | Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases. |
J Med Chem 46: 674-6 (2003) | Enanta Pharmaceuticals | 2D 3D TSV |
| 12593645 | 2 | In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist. |
J Med Chem 46: 670-3 (2003) | Pfizer Inc | 2D 3D TSV |
| 12593644 | 27 | Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists. |
J Med Chem 46: 666-9 (2003) | Tsukuba Research Institute | 2D 3D TSV |
| 12573694 | 13 | Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation. |
Chem Biol 10: 15-24 (2003) | Tohoku University | 2D 3D TSV |
| 12570387 | 60 | Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands. |
J Med Chem 46: 646-9 (2003) | Università degli Studi di Bari | 2D 3D TSV |
| 12570386 | 15 | Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity. |
J Med Chem 46: 642-5 (2003) | National Institute on Drug Abuse | 2D 3D TSV |
| 12570383 | 46 | 3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors. |
J Med Chem 46: 623-33 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12570381 | 15 | Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists. |
J Med Chem 46: 601-8 (2003) | Columbia University | 2D 3D TSV |
| 12570380 | 34 | Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and as potential antitumor agents. |
J Med Chem 46: 591-600 (2003) | Duquesne University | 2D 3D TSV |
| 12570379 | 6 | Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity. |
J Med Chem 46: 584-90 (2003) | University Centre for Pharmacy | 2D 3D TSV |
| 12570378 | 6 | Design, synthesis, and biological evaluation of a series of fluoroquinoanthroxazines with contrasting dual mechanisms of action against topoisomerase II and G-quadruplexes. |
J Med Chem 46: 571-83 (2003) | The University of Arizona | 2D 3D TSV |
| 12570376 | 20 | Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. |
J Med Chem 46: 542-57 (2003) | Universit£ de Lille II | 2D 3D TSV |
| 12570371 | 33 | Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5. |
J Med Chem 46: 486-98 (2003) | Aventis Pharma Deutschland GmbH | 2D 3D TSV |
| 12570369 | 60 | Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines. |
J Med Chem 46: 461-73 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12570368 | 9 | Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. |
J Med Chem 46: 457-60 (2003) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12570367 | 9 | Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. |
J Med Chem 46: 453-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12570021 | 16 | Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors. |
Fundam Clin Pharmacol 16: 317-23 (2002) | Shinshu University | 2D 3D TSV |
| 12569305 | 12 | Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. |
Anticancer Drugs 14: 175-81 (2003) | Korea Research Institute of Chemical Technology | 2D 3D TSV |
| 12565974 | 3 | Condensed aromatic peptide family of microbial metabolites, inhibitors of CD28-CD80 interactions. |
Bioorg Med Chem Lett 13: 573-5 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12565973 | 33 | Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides. |
Bioorg Med Chem Lett 13: 567-71 (2003) | Schering-Plough Research Institute | 2D 3D TSV |
| 12565972 | 69 | Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors. |
Bioorg Med Chem Lett 13: 561-6 (2003) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12565970 | 44 | Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents. |
Bioorg Med Chem Lett 13: 553-6 (2003) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
| 12565969 | 36 | Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues. |
Bioorg Med Chem Lett 13: 547-51 (2003) | Bristol-Myers Squibb PRI | 2D 3D TSV |
| 12565968 | 40 | Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series. |
Bioorg Med Chem Lett 13: 543-6 (2003) | Bristol-Myers Squibb PRI | 2D 3D TSV |
| 12565966 | 33 | Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists. |
Bioorg Med Chem Lett 13: 533-8 (2003) | Bristol-Myers Squibb Pharmaceuticals | 2D 3D TSV |
| 12565965 | 45 | Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans. |
Bioorg Med Chem Lett 13: 529-32 (2003) | Southern Research Institute | 2D 3D TSV |
| 12565964 | 4 | 5-Azidoepibatidine: an exceptionally potent photoaffinity ligand for neuronal alpha 4 beta 2 and alpha 7 nicotinic acetylcholine receptors. |
Bioorg Med Chem Lett 13: 525-7 (2003) | University of California | 2D 3D TSV |
| 12565962 | 41 | Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors. |
Bioorg Med Chem Lett 13: 513-7 (2003) | University of Michigan | 2D 3D TSV |
| 12565961 | 177 | Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors. |
Bioorg Med Chem Lett 13: 507-11 (2003) | Berlex Biosciences | 2D 3D TSV |
| 12565960 | 33 | Thiophene-based vitronectin receptor antagonists. |
Bioorg Med Chem Lett 13: 503-6 (2003) | Shire BioChem Inc | 2D 3D TSV |
| 12565959 | 9 | 1,4-Diazepane-2-ones as novel inhibitors of LFA-1. |
Bioorg Med Chem Lett 13: 499-502 (2003) | Novartis Institute for BioMedical Research | 2D 3D TSV |
| 12565955 | 33 | 2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs). |
Bioorg Med Chem Lett 13: 479-83 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12565952 | 26 | p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones. |
Bioorg Med Chem Lett 13: 467-70 (2003) | Merck & Co. | 2D 3D TSV |
| 12565948 | 120 | Modelling of carbonic anhydrase inhibitory activity of sulfonamides using molecular negentropy. |
Bioorg Med Chem Lett 13: 447-53 (2003) | A.P.S. University | 2D 3D TSV |
| 12565947 | 1 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
Bioorg Med Chem Lett 13: 443-6 (2003) | Università di Messina | 2D 3D TSV |
| 12565946 | 51 | Discovery of orally bioavailable NK1 receptor antagonists. |
Bioorg Med Chem Lett 13: 437-42 (2003) | UCB Pharma SA | 2D 3D TSV |
| 12565944 | 47 | 1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains. |
Bioorg Med Chem Lett 13: 427-31 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12565943 | 43 | A series of 2(Z)-2-benzylidene-6,7-dihydroxybenzofuran-3[2H]-ones as inhibitors of chorismate synthase. |
Bioorg Med Chem Lett 13: 423-6 (2003) | PanTherix Ltd. | 2D 3D TSV |
| 12565941 | 27 | 2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors. |
Bioorg Med Chem Lett 13: 413-7 (2003) | AmorePacific Corporation | 2D 3D TSV |
| 12565939 | 38 | SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition. |
Bioorg Med Chem Lett 13: 405-8 (2003) | Solvay Pharma | 2D 3D TSV |
| 12565935 | 5 | Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors. |
Bioorg Med Chem Lett 13: 387-9 (2003) | The Oxford Centre for Molecular Sciences and The Dyson Perrins Laboratory | 2D 3D TSV |
| 12565933 | 30 | Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. |
Bioorg Med Chem Lett 13: 379-82 (2003) | Pfizer Inc | 2D 3D TSV |
| 12565931 | 37 | Nonbenzamidine tetrazole derivatives as factor Xa inhibitors. |
Bioorg Med Chem Lett 13: 369-73 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12565928 | 11 | [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. |
Bioorg Med Chem Lett 13: 351-4 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12565927 | 24 | Imidazopyrimidines, potent inhibitors of p38 MAP kinase. |
Bioorg Med Chem Lett 13: 347-50 (2003) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12565923 | 6 | Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors. |
Bioorg Med Chem Lett 13: 331-4 (2003) | Leiden University | 2D 3D TSV |
| 12565883 | 1 | AF2 interaction with Ascaris suum body wall muscle membranes involves G-protein activation. |
Biochem Biophys Res Commun 301: 456-9 (2003) | Pharmacia Corporation | 2D 3D TSV |
| 12542356 | 4 | Cationic reduction of bastadin-4 to bastadin-5. Preparation of 5-[2h]-bastadin-5 by site-specific isotopic labeling. |
J Nat Prod 66: 112-4 (2003) | University of California | 2D 3D TSV |
| 12542354 | 3 | Chemical and biological investigation of the fungus Pulveroboletus ravenelii. |
J Nat Prod 66: 103-7 (2003) | The University of Mississippi | 2D 3D TSV |
| 12542342 | 2 | Flavanone glycosides from Miconia trailii. |
J Nat Prod 66: 39-41 (2003) | University of Mississippi | 2D 3D TSV |
| 12540243 | 29 | Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction. |
J Med Chem 46: 441-4 (2003) | Johnson & Johnson Pharmaceutical Research & Development LLC | 2D 3D TSV |
| 12540241 | 5 | Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides. |
J Med Chem 46: 417-26 (2003) | Aristotle University of Thessaloniki | 2D 3D TSV |
| 12540239 | 3 | Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity. |
J Med Chem 46: 399-408 (2003) | GlaxoSmithKline | 2D 3D TSV |
| 12540236 | 11 | New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. |
J Med Chem 46: 364-73 (2003) | Georgetown University Medical Center | 2D 3D TSV |
| 12540233 | 16 | 3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor. |
J Med Chem 46: 353-5 (2003) | Pfizer Inc | 2D 3D TSV |
| 12540232 | 53 | Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones. |
J Med Chem 46: 349-52 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12540231 | 39 | Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling. |
J Med Chem 46: 345-8 (2003) | MRL Rome | 2D 3D TSV |
| 12540230 | 18 | 5-HT4 receptor ligands: applications and new prospects. |
J Med Chem 46: 319-44 (2003) | Paris-Sud University | 2D 3D TSV |
| 12538898 | 12 | Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species. |
Protein Sci 12: 349-60 (2003) | GSK | 2D 3D TSV |
| 12538838 | 14 | Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor. |
J Pharmacol Exp Ther 304: 818-26 (2003) | Taisho Pharmaceutical Co. | 2D 3D TSV |
| 12538837 | 2 | Agmatine is efficiently transported by non-neuronal monoamine transporters extraneuronal monoamine transporter (EMT) and organic cation transporter 2 (OCT2). |
J Pharmacol Exp Ther 304: 810-7 (2003) | University of Cologne | 2D 3D TSV |
| 12538813 | 1 | Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. |
J Pharmacol Exp Ther 304: 610-6 (2003) | Kitasato University | 2D 3D TSV |
| 12538807 | 4 | Interaction of cysteine conjugates with human and rabbit organic anion transporter 1. |
J Pharmacol Exp Ther 304: 560-6 (2003) | University of Arizona | 2D 3D TSV |
| 12534346 | 22 | The specificities of protein kinase inhibitors: an update. |
Biochem J 371: 199-204 (2003) | University of Dundee | 2D 3D TSV |
| 12534275 | 32 | A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance. |
Biochemistry 42: 631-8 (2003) | The Johns Hopkins University | 2D 3D TSV |
| 12533678 | 10 | Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists. |
Mol Cancer Ther 2: 105-12 (2003) | Japanese Foundation for Cancer Research | 2D 3D TSV |
| 12527336 | 21 | Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. |
Biochem Pharmacol 65: 435-40 (2003) | Aventis Pharma | 2D 3D TSV |
| 12526824 | 2 | Prodrugs of purine and pyrimidine analogues for the intestinal di/tri-peptide transporter PepT1: affinity for hPepT1 in Caco-2 cells, drug release in aqueous media and in vitro metabolism. |
J Control Release 86: 279-92 (2003) | The Royal Danish School of Pharmacy | 2D 3D TSV |
| 12523936 | 19 | Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). |
Biochem J 371: 361-7 (2003) | The Netherlands Cancer Institute | 2D 3D TSV |
| 12519069 | 60 | The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole. |
J Med Chem 46: 314-7 (2003) | University of Bath | 2D 3D TSV |
| 12519068 | 32 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
J Med Chem 46: 310-3 (2003) | University of Firenze | 2D 3D TSV |
| 12519067 | 27 | Discovery of a long-chain carbamoyl aminocarnitine derivative, a reversible carnitine palmitoyltransferase inhibitor with antiketotic and antidiabetic activity. |
J Med Chem 46: 303-9 (2003) | Sigma Tau Pharmaceutical Industries S.p.A. | 2D 3D TSV |
| 12519065 | 243 | Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
J Med Chem 46: 265-83 (2003) | H. Lundbeck A/S | 2D 3D TSV |
| 12519064 | 48 | Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists. |
J Med Chem 46: 255-64 (2003) | F. Hoffmann-La Roche Ltd. | 2D 3D TSV |
| 12519063 | 5 | Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems. |
J Med Chem 46: 244-54 (2003) | National Cancer Institute-Frederick | 2D 3D TSV |
| 12519062 | 11 | Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain. |
J Med Chem 46: 237-43 (2003) | University of Pennsylvania | 2D 3D TSV |
| 12519061 | 145 | Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. |
J Med Chem 46: 222-36 (2003) | Faculte de Medecine et de Pharmacie | 2D 3D TSV |
| 12519059 | 10 | Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. |
J Med Chem 46: 210-3 (2003) | Pfizer Inc | 2D 3D TSV |
| 12519058 | 8 | Potential tumor-selective nitroimidazolylmethyluracil prodrug derivatives: inhibitors of the angiogenic enzyme thymidine phosphorylase. |
J Med Chem 46: 207-9 (2003) | University of Manchester | 2D 3D TSV |
| 12519057 | 22 | 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
J Med Chem 46: 204-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12517147 | 6 | Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity. |
J Am Chem Soc 125: 363-73 (2003) | Weizmann Institute of Science | 2D 3D TSV |
| 12513698 | 6 | Activity of opioid ligands in cells expressing cloned mu opioid receptors. |
BMC Pharmacol 3: 1 (2003) | Molecular Research Institute | 2D 3D TSV |
| 12502370 | 39 | New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor. |
J Med Chem 46: 161-8 (2002) | Universit£ di Pisa | 2D 3D TSV |
| 12502369 | 8 | 8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases. |
J Med Chem 46: 155-60 (2002) | Industrial Research Limited | 2D 3D TSV |
| 12502367 | 17 | New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization. |
J Med Chem 46: 138-47 (2002) | Université de Caen | 2D 3D TSV |
| 12502366 | 82 | Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. |
J Med Chem 46: 125-37 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12502365 | 41 | Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. |
J Med Chem 46: 113-24 (2002) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
| 12502364 | 17 | Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence. |
J Med Chem 46: 105-12 (2002) | Kissei Pharmaceutical Company Ltd | 2D 3D TSV |
| 12502361 | 53 | Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities. |
J Med Chem 46: 74-86 (2002) | Vrije Universiteit | 2D 3D TSV |
| 12502360 | 23 | Hydantoin-substituted 4,6-dichloroindole-2-carboxylic acids as ligands with high affinity for the glycine binding site of the NMDA receptor. |
J Med Chem 46: 64-73 (2002) | Johannes Gutenberg-Universität | 2D 3D TSV |
| 12502359 | 70 | Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2). |
J Med Chem 46: 49-63 (2002) | Wyeth Research | 2D 3D TSV |
| 12502358 | 126 | The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity. |
J Med Chem 46: 34-48 (2002) | Universit£ de Montr£al | 2D 3D TSV |
| 12502354 | 30 | Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding. |
J Med Chem 46: 9-11 (2002) | Amgen Inc | 2D 3D TSV |
| 12502352 | 28 | Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors. |
J Med Chem 46: 1-4 (2002) | Universit£ di Siena | 2D 3D TSV |
| 12502345 | 1 | Sodium 1-(12-hydroxy)octadecanyl sulfate, an MMP2 inhibitor, isolated from a tunicate of the family Polyclinidae. |
J Nat Prod 65: 1936-8 (2002) | the University of Tokyo | 2D 3D TSV |
| 12502331 | 28 | New polyhydroxylated pyrrolidine, piperidine, and pyrrolizidine alkaloids from Scilla sibirica. |
J Nat Prod 65: 1875-81 (2002) | Hokuriku University | 2D 3D TSV |
| 12502307 | 6 | Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis. |
J Nat Prod 65: 1749-53 (2002) | Université de Lausanne | 2D 3D TSV |
| 12498885 | 9 | Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition. |
Chem Biol 9: 1323-8 (2002) | Massachusetts Institute of Technology | 2D 3D TSV |
| 12482445 | 16 | Synthesis and evaluation of phosphoramidate amino acid-based inhibitors of sialyltransferases. |
Bioorg Med Chem Lett 13: 301-4 (2002) | University of Colorado | 2D 3D TSV |
| 12482444 | 38 | Design and synthesis of factor Xa inhibitors and their prodrugs. |
Bioorg Med Chem Lett 13: 297-300 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12482442 | 13 | CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine. |
Bioorg Med Chem Lett 13: 289-91 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12482441 | 45 | Development of a presynaptic 5-HT1A antagonist. |
Bioorg Med Chem Lett 13: 285-8 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12482439 | 51 | Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase. |
Bioorg Med Chem Lett 13: 277-80 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12482438 | 50 | p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold. |
Bioorg Med Chem Lett 13: 273-6 (2003) | Merck Research Laboratories | 2D 3D TSV |
| 12482437 | 42 | Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists. |
Bioorg Med Chem Lett 13: 269-71 (2003) | Pfizer Inc | 2D 3D TSV |
| 12482435 | 75 | Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid. |
Bioorg Med Chem Lett 13: 261-4 (2002) | Ligand Pharmaceuticals Inc | 2D 3D TSV |
| 12482434 | 52 | Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template. |
Bioorg Med Chem Lett 13: 257-60 (2002) | Novo Nordisk A/S | 2D 3D TSV |
| 12482429 | 10 | Synthesis of non-competitive inhibitors of sphingomyelinases with significant activity. |
Bioorg Med Chem Lett 13: 229-36 (2002) | Tokyo University of Pharmacy & Life Science | 2D 3D TSV |
| 12482427 | 36 | 4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. |
Bioorg Med Chem Lett 13: 217-22 (2003) | University of Newcastle | 2D 3D TSV |
| 12482425 | 20 | Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties. |
Bioorg Med Chem Lett 13: 209-12 (2002) | Institut Henri Beaufour | 2D 3D TSV |
| 12482423 | 6 | [18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). |
Bioorg Med Chem Lett 13: 201-4 (2002) | National Institute of Radiological Sciences | 2D 3D TSV |
| 12482418 | 18 | New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. |
Bioorg Med Chem Lett 13: 175-8 (2002) | University of Santiago | 2D 3D TSV |
| 12482417 | 23 | alpha1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus. |
Bioorg Med Chem Lett 13: 171-3 (2002) | Università di Pisa | 2D 3D TSV |
| 12482416 | 52 | Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones. |
Bioorg Med Chem Lett 13: 165-9 (2002) | BASF AG | 2D 3D TSV |
| 12482415 | 30 | Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'. |
Bioorg Med Chem Lett 13: 161-4 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12477359 | 78 | Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide. |
J Med Chem 45: 5755-75 (2002) | Novo Nordisk A/S | 2D 3D TSV |
| 12477358 | 40 | Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors. |
J Med Chem 45: 5745-54 (2002) | The Royal Danish School of Pharmacy | 2D 3D TSV |
| 12477357 | 96 | Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position. |
J Med Chem 45: 5736-44 (2002) | University of Florida | 2D 3D TSV |
| 12477356 | 137 | Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands. |
J Med Chem 45: 5727-35 (2002) | Universit£ degli Studi di Bari | 2D 3D TSV |
| 12477354 | 8 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
J Med Chem 45: 5710-20 (2002) | Università degli Studi di Firenze | 2D 3D TSV |
| 12477352 | 85 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
J Med Chem 45: 5687-93 (2002) | Novartis Pharma AG | 2D 3D TSV |
| 12477351 | 41 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
J Med Chem 45: 5671-86 (2002) | Bulgarian Academy of Sciences | 2D 3D TSV |
| 12477350 | 47 | Metal-dependent inhibition of HIV-1 integrase. |
J Med Chem 45: 5661-70 (2002) | University of Southern California | 2D 3D TSV |
| 12477349 | 26 | In silico and NMR identification of inhibitors of the IGF-I and IGF-binding protein-5 interaction. |
J Med Chem 45: 5655-60 (2002) | Institute for Biochemistry | 2D 3D TSV |
| 12477347 | 16 | Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin. |
J Med Chem 45: 5640-8 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12477346 | 30 | NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability. |
J Med Chem 45: 5628-39 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12477343 | 8 | Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist. |
J Med Chem 45: 5617-9 (2002) | University of Maryland | 2D 3D TSV |
| 12477342 | 27 | 2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery. |
J Med Chem 45: 5609-16 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12475240 | 2 | Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor. |
Biochemistry 41: 14916-14924 (2002) | UCLA and the Wadsworth Veterans Administration Hospital | 2D 3D TSV |
| 12472777 | 3 | Urate transport via human PAH transporter hOAT1 and its gene structure. |
Kidney Int 63: 143-55 (2003) | Jikei University School of Medicine | 2D 3D TSV |
| 12467634 | 67 | 3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors. |
Bioorg Med Chem Lett 13: 139-41 (2002) | currently NAEJA Pharmaceutical Inc. | 2D 3D TSV |
| 12467633 | 58 | Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution. |
Bioorg Med Chem Lett 13: 133-7 (2002) | Roche Research Center | 2D 3D TSV |
| 12467632 | 13 | Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands. |
Bioorg Med Chem Lett 13: 129-31 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12467631 | 32 | Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands. |
Bioorg Med Chem Lett 13: 125-8 (2003) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12467630 | 25 | 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains. |
Bioorg Med Chem Lett 13: 119-23 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12467628 | 118 | Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B. |
Bioorg Med Chem Lett 13: 111-3 (2002) | Banyu Tsukuba Research Institute | 2D 3D TSV |
| 12467627 | 7 | Design of novel N-(2,4-dioxo-1,2,3,4-tetrahydro-thieno[3,2-d]pyrimidin-7-yl)-guanidines as thymidine phosphorylase inhibitors, and flexible docking to a homology model. |
Bioorg Med Chem Lett 13: 107-10 (2002) | Attenuon LLC | 2D 3D TSV |
| 12467625 | 32 | N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors. |
Bioorg Med Chem Lett 13: 97-100 (2002) | Chinese Academy of Sciences | 2D 3D TSV |
| 12467624 | 9 | Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere. |
Bioorg Med Chem Lett 13: 93-6 (2002) | Kyoto Pharmaceutical University | 2D 3D TSV |
| 12467623 | 38 | Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3. |
Bioorg Med Chem Lett 13: 87-91 (2003) | Nippon Roche Research Center | 2D 3D TSV |
| 12467622 | 5 | Fluorescent bioprobes for visualization of puromycin-sensitive aminopeptidase in living cells. |
Bioorg Med Chem Lett 13: 83-6 (2002) | The University of Tokyo | 2D 3D TSV |
| 12467619 | 12 | Rational approaches towards reversible inhibition of type B monoamine oxidase. Design and evaluation of a novel 5H-Indeno[1,2-c]pyridazin-5-one derivative. |
Bioorg Med Chem Lett 13: 69-73 (2002) | Facultés Universitaires Notre-Dame de la Paix | 2D 3D TSV |
| 12467617 | 17 | New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. |
Bioorg Med Chem Lett 13: 61-4 (2003) | Meiji Seika Kaisha, Ltd | 2D 3D TSV |
| 12467613 | 15 | Homologues and isomers of noladin ether, a putative novel endocannabinoid: interaction with rat cannabinoid CB(1) receptors. |
Bioorg Med Chem Lett 13: 43-6 (2002) | DiSCAFF | 2D 3D TSV |
| 12467612 | 1 | Synthesis and gamma-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres. |
Bioorg Med Chem Lett 13: 37-41 (2002) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
| 12467610 | 1 | Identification of a stable chymase inhibitor using a pharmacophore-Based database search. |
Bioorg Med Chem Lett 13: 25-9 (2002) | Toa Eiyo Ltd | 2D 3D TSV |
| 12466002 | 3 | Etoricoxib. |
Drugs 62: 2637 (2002) | Adis International Limited | 2D 3D TSV |
| 12460667 | 18 | Hybrid ubiquinone: novel inhibitor of mitochondrial complex I. |
Biochim Biophys Acta 1556: 106-12 (2002) | Kyoto University | 2D 3D TSV |
| 12459025 | 84 | Use of ab initio calculations to predict the biological potency of carboxylesterase inhibitors. |
J Med Chem 45: 5576-93 (2002) | University of California | 2D 3D TSV |
| 12459024 | 3 | Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 1. |
J Med Chem 45: 5564-75 (2002) | Dainippon Pharmaceutical Co., Ltd. | 2D 3D TSV |
| 12459023 | 46 | Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore. |
J Med Chem 45: 5556-63 (2002) | University of Cagliari | 2D 3D TSV |
| 12459018 | 6 | Crystal structures of dipeptides containing the Dmt-Tic pharmacophore. |
J Med Chem 45: 5506-13 (2002) | National Institute of Environmental Health Sciences | 2D 3D TSV |
| 12459017 | 132 | A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta. |
J Med Chem 45: 5492-505 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12459015 | 68 | Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors. |
J Med Chem 45: 5471-82 (2002) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
| 12459011 | 94 | Relationships between structure and interaction kinetics for HIV-1 protease inhibitors. |
J Med Chem 45: 5430-9 (2002) | Uppsala University | 2D 3D TSV |
| 12459007 | 13 | Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists. |
J Med Chem 45: 5415-8 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12444712 | 3 | Total synthesis and biological evaluation of (5Z,9Z)-5,9-hexadecadienoic acid, an inhibitor of human topoisomerase I. |
J Nat Prod 65: 1715-8 (2002) | University of Puerto Rico | 2D 3D TSV |
| 12444711 | 3 | Aldehyde dehydrogenase inhibitors from the mushroom Clitocybe clavipes. |
J Nat Prod 65: 1712-4 (2002) | Shizuoka University | 2D 3D TSV |
| 12444693 | 5 | Triterpenoid constituents isolated from the bark of Abies sachalinensis. |
J Nat Prod 65: 1657-9 (2002) | Osaka University of Pharmaceutical Sciences | 2D 3D TSV |
| 12444671 | 10 | Antioxidant and free-radical scavenging activity of constituents of the leaves of Tachigalia paniculata. |
J Nat Prod 65: 1526-9 (2002) | Università di Salerno | 2D 3D TSV |
| 12444669 | 10 | Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay. |
J Nat Prod 65: 1517-21 (2002) | Uppsala University | 2D 3D TSV |
| 12443792 | 51 | Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists. |
Bioorg Med Chem Lett 12: 3635-9 (2002) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
| 12443791 | 14 | Inhibition of amine oxidases activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives. |
Bioorg Med Chem Lett 12: 3629-33 (2002) | Sapienza University of Rome | 2D 3D TSV |
| 12443790 | 3 | Silanediol-based inhibitor of thermolysin. |
Bioorg Med Chem Lett 12: 3625-7 (2002) | State University of New York | 2D 3D TSV |
| 12443787 | 2 | Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporter. |
Bioorg Med Chem Lett 12: 3611-3 (2002) | Institutet | 2D 3D TSV |
| 12443785 | 4 | Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides. |
Bioorg Med Chem Lett 12: 3601-4 (2002) | Université de Lille 2 | 2D 3D TSV |
| 12443784 | 12 | Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the metal binding group. |
Bioorg Med Chem Lett 12: 3595-9 (2002) | British Biotech Pharmaceuticals Limited | 2D 3D TSV |
| 12443781 | 22 | Novel 1',1'-chain substituted Delta(8)-tetrahydrocannabinols. |
Bioorg Med Chem Lett 12: 3583-6 (2002) | National Hellenic Research Foundation | 2D 3D TSV |
| 12443779 | 44 | 2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties. |
Bioorg Med Chem Lett 12: 3573-7 (2002) | Janssen-Cilag S.A. | 2D 3D TSV |
| 12443777 | 63 | Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators. |
Bioorg Med Chem Lett 12: 3565-7 (2002) | Biovitrum AB | 2D 3D TSV |
| 12443774 | 12 | Natural and synthetic geiparvarins are strong and selective MAO-B inhibitors. Synthesis and SAR studies. |
Bioorg Med Chem Lett 12: 3551-5 (2002) | University of Bari | 2D 3D TSV |
| 12443771 | 19 | Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics. |
Bioorg Med Chem Lett 12: 3537-41 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12438541 | 27 | SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization. |
J Pharmacol Exp Ther 303: 1171-9 (2002) | Sanofi-Synthélabo Recherche | 2D 3D TSV |
| 12438527 | 3 | Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin. |
J Pharmacol Exp Ther 303: 1052-60 (2002) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
| 12438526 | 1 | [3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. |
J Pharmacol Exp Ther 303: 1044-51 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12438515 | 20 | The cation transporters rOCT1 and rOCT2 interact with bicarbonate but play only a minor role for amantadine uptake into rat renal proximal tubules. |
J Pharmacol Exp Ther 303: 959-68 (2002) | University of Manitoba | 2D 3D TSV |
| 12431845 | 84 | Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder. |
Neuropsychopharmacology 27: 699-711 (2002) | Eli Lilly and Company | 2D 3D TSV |
| 12431069 | 11 | Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents. |
J Med Chem 45: 5410-3 (2002) | Università di Messina | 2D 3D TSV |
| 12431066 | 6 | Adenosine 5'-O-(1-boranotriphosphate) derivatives as novel P2Y(1) receptor agonists. |
J Med Chem 45: 5384-96 (2002) | Bar-Ilan University | 2D 3D TSV |
| 12431065 | 72 | Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans. |
J Med Chem 45: 5378-83 (2002) | University of Innsbruck | 2D 3D TSV |
| 12431064 | 43 | Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-[2-[(3-substituted)-1-azetidinyl]ethyl]-2-piperidones. 1. Selective antagonists of the neurokinin-2 receptor. |
J Med Chem 45: 5365-77 (2002) | Pfizer Inc | 2D 3D TSV |
| 12431063 | 8 | Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes. |
J Med Chem 45: 5358-64 (2002) | Free University of Berlin | 2D 3D TSV |
| 12431062 | 33 | Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist. |
J Med Chem 45: 5353-7 (2002) | Universit£ de Montr£al | 2D 3D TSV |
| 12431059 | 27 | Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides. |
J Med Chem 45: 5321-9 (2002) | National Research Council of Canada | 2D 3D TSV |
| 12431057 | 8 | Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles. |
J Med Chem 45: 5303-10 (2002) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12431056 | 9 | Sulfamide-based inhibitors for carboxypeptidase A. Novel type transition state analogue inhibitors for zinc proteases. |
J Med Chem 45: 5295-302 (2002) | Pohang University of Science and Technology | 2D 3D TSV |
| 12431055 | 52 | Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors. |
J Med Chem 45: 5287-94 (2002) | University of Arizona | 2D 3D TSV |
| 12431054 | 28 | Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints. |
J Med Chem 45: 5280-6 (2002) | Purdue Pharma LP | 2D 3D TSV |
| 12431053 | 293 | Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease. |
J Med Chem 45: 5260-79 (2002) | Teva Pharmaceutical Industries | 2D 3D TSV |
| 12431052 | 22 | Molecular docking and 3D-QSAR studies on gag peptide analogue inhibitors interacting with human cyclophilin A. |
J Med Chem 45: 5249-59 (2002) | Chinese Academy of Sciences | 2D 3D TSV |
| 12431051 | 114 | Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2). |
J Med Chem 45: 5233-48 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12431050 | 76 | Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern. |
J Med Chem 45: 5224-32 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12419810 | 6 | Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight. |
J Biol Chem 278: 1831-6 (2003) | University of Padova | 2D 3D TSV |
| 12419391 | 8 | A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists. |
Bioorg Med Chem Lett 12: 3491-5 (2002) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12419390 | 37 | New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles. |
Bioorg Med Chem Lett 12: 3487-90 (2002) | Wyeth Research | 2D 3D TSV |
| 12419389 | 13 | Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements. |
Bioorg Med Chem Lett 12: 3483-6 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12419388 | 25 | Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification. |
Bioorg Med Chem Lett 12: 3479-82 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12419386 | 5 | Synthesis of [difluoro-(3-alkenylphenyl)-methyl]-phosphonic acids on non-crosslinked polystyrene and their evaluation as inhibitors of PTP1B. |
Bioorg Med Chem Lett 12: 3471-4 (2002) | University of Waterloo | 2D 3D TSV |
| 12419385 | 48 | The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists. |
Bioorg Med Chem Lett 12: 3467-70 (2002) | Agouron Pharmaceuticals Inc | 2D 3D TSV |
| 12419382 | 51 | Six-membered cyclic ureas as HIV-1 protease inhibitors: a QSAR study based on CODESSA PRO approach. Quantitative structure-activity relationships. |
Bioorg Med Chem Lett 12: 3453-7 (2002) | University of Florida | 2D 3D TSV |
| 12419381 | 95 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
Bioorg Med Chem Lett 12: 3449-52 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12419380 | 24 | Trifluoromethyl ketones as inhibitors of histone deacetylase. |
Bioorg Med Chem Lett 12: 3443-7 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12419377 | 5 | Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease. |
Bioorg Med Chem Lett 12: 3431-3 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12419375 | 21 | Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists. |
Bioorg Med Chem Lett 12: 3421-4 (2002) | Bayer Research Center | 2D 3D TSV |
| 12419374 | 45 | 6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S. |
Bioorg Med Chem Lett 12: 3417-9 (2002) | currently NAEJA Pharmaceutical Inc. | 2D 3D TSV |
| 12419373 | 18 | Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors. |
Bioorg Med Chem Lett 12: 3413-5 (2002) | currently NAEJA Pharmaceutical Inc. | 2D 3D TSV |
| 12419367 | 5 | Natural PTP1B inhibitors from Broussonetia papyrifera. |
Bioorg Med Chem Lett 12: 3387-90 (2002) | Chinese Academy of Sciences | 2D 3D TSV |
| 12419366 | 27 | Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase. |
Bioorg Med Chem Lett 12: 3383-6 (2002) | Pharmacia Corporation | 2D 3D TSV |
| 12419362 | 19 | Chemical modification of reveromycin A and its biological activities. |
Bioorg Med Chem Lett 12: 3363-6 (2002) | RIKEN (The Institute of Physical and Chemical Research) | 2D 3D TSV |
| 12419361 | 23 | Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease. |
Bioorg Med Chem Lett 12: 3359-62 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12408728 | 6 | Spectral and crystallographic study of pyridinic analogues of nimesulide: determination of the active form of methanesulfonamides as COX-2 selective inhibitors. |
J Med Chem 45: 5182-5 (2002) | Université de Liège | 2D 3D TSV |
| 12408727 | 38 | Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates. |
J Med Chem 45: 5173-81 (2002) | Duquesne University | 2D 3D TSV |
| 12408725 | 1 | Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. |
J Med Chem 45: 5150-6 (2002) | Forschungszentrum Jülich GmbH | 2D 3D TSV |
| 12408724 | 79 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
J Med Chem 45: 5136-49 (2002) | University of Liège | 2D 3D TSV |
| 12408719 | 21 | Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB). |
J Med Chem 45: 5081-9 (2002) | Daiichi Fine Chemical Co. Ltd. | 2D 3D TSV |
| 12408715 | 97 | Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor. |
J Med Chem 45: 5043-51 (2002) | Neurogen Corporation | 2D 3D TSV |
| 12408713 | 54 | Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists. |
J Med Chem 45: 5030-6 (2002) | Università di Pisa | 2D 3D TSV |
| 12408711 | 112 | Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design. |
J Med Chem 45: 5005-22 (2002) | Sunesis Pharmaceuticals | 2D 3D TSV |
| 12408710 | 2 | Thrombin inhibition by novel benzamidine derivatives: a free-energy perturbation study. |
J Med Chem 45: 4995-5004 (2002) | Universidade Federal do Rio de Janeiro | 2D 3D TSV |
| 12408709 | 11 | Synthesis, solution structure, and biological evaluation of urokinase type plasminogen activator (uPA)-derived receptor binding domain mimetics. |
J Med Chem 45: 4984-94 (2002) | Technische Universität München | 2D 3D TSV |
| 12408708 | 7 | Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum. |
J Med Chem 45: 4975-83 (2002) | The University of Liverpool | 2D 3D TSV |
| 12408707 | 32 | Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure. |
J Med Chem 45: 4961-74 (2002) | Pfizer Inc | 2D 3D TSV |
| 12408705 | 73 | Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships. |
J Med Chem 45: 4954-7 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12408704 | 3 | Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954). |
J Med Chem 45: 4950-3 (2002) | ACADIA Pharmaceuticals Inc. | 2D 3D TSV |
| 12404239 | 6 | The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. |
Gastroenterology 123: 1649-58 (2002) | King's College Hospital | 2D 3D TSV |
| 12401496 | 89 | Crystal structures of Candida albicans N-myristoyltransferase with two distinct inhibitors. |
Chem Biol 9: 1119-28 (2002) | Nippon Roche Research Center | 2D 3D TSV |
| 12398550 | 1 | Panepophenanthrin, from a mushroom strain, a novel inhibitor of the ubiquitin-activating enzyme. |
J Nat Prod 65: 1491-3 (2002) | Institute of Microbial Chemistry | 2D 3D TSV |
| 12398547 | 9 | Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors. |
J Nat Prod 65: 1479-85 (2002) | University of Bonn | 2D 3D TSV |
| 12398542 | 6 | Constituents of the stigmas of Crocus sativus and their tyrosinase inhibitory activity. |
J Nat Prod 65: 1452-6 (2002) | National Cheng Kung University | 2D 3D TSV |
| 12392747 | 36 | SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. |
Bioorg Med Chem Lett 12: 3341-4 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12392746 | 18 | 3-Hydroxy-4-methyl-5-pentyl-2-iminopyrrolidine: a potent and highly selective inducible nitric oxide synthase inhibitor. |
Bioorg Med Chem Lett 12: 3337-9 (2002) | Pharmacia | 2D 3D TSV |
| 12392744 | 36 | Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists. |
Bioorg Med Chem Lett 12: 3329-32 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12392743 | 17 | Capped dipeptide alpha-ketoacid inhibitors of the HCV NS3 protease. |
Bioorg Med Chem Lett 12: 3325-8 (2002) | IRBM, MRL Rome | 2D 3D TSV |
| 12392741 | 7 | Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile. |
Bioorg Med Chem Lett 12: 3317-20 (2002) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12392739 | 41 | Novel human histamine H(3) receptor antagonists. |
Bioorg Med Chem Lett 12: 3309-12 (2002) | Johnson and Johnson Pharmaceutical Research and Development | 2D 3D TSV |
| 12392738 | 15 | The TosMIC approach to 3-(oxazol-5-yl) indoles: application to the synthesis of indole-based IMPDH inhibitors. |
Bioorg Med Chem Lett 12: 3305-8 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12392735 | 30 | Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists. |
Bioorg Med Chem Lett 12: 3291-6 (2002) | Institut de Recherches Servier | 2D 3D TSV |
| 12392734 | 5 | Identification of novel inhibitors of fibroblast growth factor (FGF-2) binding to heparin and endothelial cell survival from a structurally diverse carbohybrid library. |
Bioorg Med Chem Lett 12: 3287-90 (2002) | University College Dublin | 2D 3D TSV |
| 12392733 | 13 | Synthesis and biological activity of olomoucine II. |
Bioorg Med Chem Lett 12: 3283-6 (2002) | Palack£ University and Institute of Experimental Botany | 2D 3D TSV |
| 12392732 | 5 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
Bioorg Med Chem Lett 12: 3279-82 (2002) | Pfizer Inc | 2D 3D TSV |
| 12392730 | 10 | Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer. |
Bioorg Med Chem Lett 12: 3271-3 (2002) | Kyorin Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12388666 | 301 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
J Pharmacol Exp Ther 303: 791-804 (2002) | Institut de Recherches Servier | 2D 3D TSV |
| 12388623 | 149 | Elucidation of the vasoactive intestinal peptide pharmacophore for VPAC(2) receptors in human and rat and comparison to the pharmacophore for VPAC(1) receptors. |
J Pharmacol Exp Ther 303: 445-60 (2002) | NIH | 2D 3D TSV |
| 12383018 | 46 | Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3. |
J Med Chem 45: 4923-30 (2002) | Pharmazeutisches Institut der Universit£t Freiburg | 2D 3D TSV |
| 12383017 | 7 | Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide. |
J Med Chem 45: 4913-22 (2002) | Eisai Co., Ltd. | 2D 3D TSV |
| 12383013 | 44 | Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists. |
J Med Chem 45: 4875-87 (2002) | Universit£ degli Studi di Genova | 2D 3D TSV |
| 12383010 | 114 | Computer-aided design of selective COX-2 inhibitors: comparative molecular field analysis, comparative molecular similarity indices analysis, and docking studies of some 1,2-diarylimidazole derivatives. |
J Med Chem 45: 4847-57 (2002) | University of Hyderabad | 2D 3D TSV |
| 12383009 | 2 | Kappa-opioid receptor model in a phospholipid bilayer: molecular dynamics simulation. |
J Med Chem 45: 4838-46 (2002) | University of Catania | 2D 3D TSV |
| 12383007 | 100 | Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses. |
J Med Chem 45: 4816-27 (2002) | Chinese Academy of Sciences | 2D 3D TSV |
| 12383006 | 24 | Benzimidazole derivatives. 3. 3D-QSAR/CoMFA model and computational simulation for the recognition of 5-HT(4) receptor antagonists. |
J Med Chem 45: 4806-15 (2002) | Universidad Complutense | 2D 3D TSV |
| 12372541 | 16 | Synthesis of potent and highly selective inhibitors of human tryptase. |
Bioorg Med Chem Lett 12: 3235-8 (2002) | The Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12372540 | 21 | Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. |
Bioorg Med Chem Lett 12: 3229-33 (2002) | The Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12372538 | 22 | Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists. |
Bioorg Med Chem Lett 12: 3219-22 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12372534 | 2 | Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5. |
Bioorg Med Chem Lett 12: 3203-5 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12372533 | 69 | P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease. |
Bioorg Med Chem Lett 12: 3199-202 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12372532 | 45 | Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives. |
Bioorg Med Chem Lett 12: 3195-8 (2002) | UCB Pharma SA | 2D 3D TSV |
| 12372531 | 6 | Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity. |
Bioorg Med Chem Lett 12: 3191-3 (2002) | Daiichi Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12372530 | 76 | Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). |
Bioorg Med Chem Lett 12: 3187-90 (2002) | Bayer AG | 2D 3D TSV |
| 12372529 | 21 | Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity. |
Bioorg Med Chem Lett 12: 3183-6 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12372528 | 15 | New irreversible adenosine A(1) antagonists based on FSCPX. |
Bioorg Med Chem Lett 12: 3179-82 (2002) | Monash University (Parkville Campus) | 2D 3D TSV |
| 12372527 | 27 | Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin. |
Bioorg Med Chem Lett 12: 3175-8 (2002) | Institute for Molecular Studies | 2D 3D TSV |
| 12372525 | 2 | A mechanism-based probe for gp120-Hydrolyzing antibodies. |
Bioorg Med Chem Lett 12: 3167-70 (2002) | University of Texas-Houston Medical School | 2D 3D TSV |
| 12372524 | 74 | Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines. |
Bioorg Med Chem Lett 12: 3161-5 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12372523 | 134 | Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands. |
Bioorg Med Chem Lett 12: 3157-60 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12372522 | 51 | Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency. |
Bioorg Med Chem Lett 12: 3153-6 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12372521 | 21 | Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors. |
Bioorg Med Chem Lett 12: 3149-52 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12372520 | 37 | Synthesis and biological activity of retinoic acid receptor-alpha specific amides. |
Bioorg Med Chem Lett 12: 3145-8 (2002) | Allergan Inc | 2D 3D TSV |
| 12372519 | 22 | Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity. |
Bioorg Med Chem Lett 12: 3141-3 (2002) | Shire BioChem | 2D 3D TSV |
| 12372517 | 92 | Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease. |
Bioorg Med Chem Lett 12: 3129-33 (2002) | Celera | 2D 3D TSV |
| 12372516 | 14 | A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase. |
Bioorg Med Chem Lett 12: 3125-8 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12372513 | 102 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
Bioorg Med Chem Lett 12: 3111-5 (2002) | Neurogen Corporation | 2D 3D TSV |
| 12372512 | 239 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships. |
Bioorg Med Chem Lett 12: 3105-9 (2002) | Neurogen Corporation | 2D 3D TSV |
| 12372510 | 28 | Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives. |
Bioorg Med Chem Lett 12: 3097-9 (2002) | EGIS Pharmaceuticals Ltd. | 2D 3D TSV |
| 12372508 | 20 | Hydroxamate based inhibitors of adenylyl cyclase. Part 2: the effect of cyclic linkers on P-site binding. |
Bioorg Med Chem Lett 12: 3089-92 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12372507 | 30 | Hydroxamate based inhibitors of adenylyl cyclase. Part 1: the effect of acyclic linkers on P-site binding. |
Bioorg Med Chem Lett 12: 3085-8 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12372506 | 41 | Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. |
Bioorg Med Chem Lett 12: 3081-4 (2002) | Johnson and Johnson Pharmaceutical Research and Development | 2D 3D TSV |
| 12372505 | 120 | Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands. |
Bioorg Med Chem Lett 12: 3077-9 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12372504 | 15 | Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands. |
Bioorg Med Chem Lett 12: 3073-6 (2002) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12372503 | 76 | bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors. |
Bioorg Med Chem Lett 12: 3067-71 (2002) | University of Kentucky | 2D 3D TSV |
| 12372501 | 21 | Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1. |
Bioorg Med Chem Lett 12: 3059-62 (2002) | Novartis Institute for BioMedical Research | 2D 3D TSV |
| 12372500 | 108 | Synthesis and evaluation of potent pyrrolidine H(3) antagonists. |
Bioorg Med Chem Lett 12: 3055-8 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12372498 | 23 | alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: structure-Activity relationship. |
Bioorg Med Chem Lett 12: 3047-50 (2002) | The Ohio State University | 2D 3D TSV |
| 12372497 | 40 | Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists. |
Bioorg Med Chem Lett 12: 3041-5 (2002) | Tsukuba Research Institute | 2D 3D TSV |
| 12371880 | 66 | Solvent and guest isotope effects on complexation thermodynamics of alpha-, beta-, and 6-amino-6-deoxy-beta-cyclodextrins. |
J Am Chem Soc 124: 12361-71 (2002) | Japan Science and Technology Agency | 2D 3D TSV |
| 12365460 | 11 | 2-styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study. |
J Enzyme Inhib Med Chem 17: 45-8 (2002) | University of Porto-Rua Anibal Cunha | 2D 3D TSV |
| 12362366 | 50 | Synthesis and structure-activity relationship of the isoindolinyl benzisoxazolpiperidines as potent, selective, and orally active human dopamine D4 receptor antagonists. |
Chembiochem 3: 999-1009 (2002) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12361407 | 4 | Comparison of 3D structures and AT(1) binding properties of pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones with parent antihypertensive drug irbesartan. |
J Med Chem 45: 4794-8 (2002) | Université de Lille 2 | 2D 3D TSV |
| 12361405 | 1 | Synthesis and investigation of conformationally restricted analogues of lavendustin A as cytotoxic inhibitors of tubulin polymerization. |
J Med Chem 45: 4774-85 (2002) | Purdue University | 2D 3D TSV |
| 12361403 | 6 | Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes: epibatidine analogues. |
J Med Chem 45: 4755-61 (2002) | Research Triangle Institute | 2D 3D TSV |
| 12361402 | 10 | The effect of exchanging various substituents at the 2-position of 2-methoxyestradiol on cytotoxicity in human cancer cell cultures and inhibition of tubulin polymerization. |
J Med Chem 45: 4748-54 (2002) | Purdue University | 2D 3D TSV |
| 12361401 | 60 | Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. |
J Med Chem 45: 4737-47 (2002) | Salk Institute | 2D 3D TSV |
| 12361399 | 17 | Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. |
J Med Chem 45: 4724-31 (2002) | Universita di Camerino | 2D 3D TSV |
| 12361398 | 19 | New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine). |
J Med Chem 45: 4716-23 (2002) | University of Pennsylvania | 2D 3D TSV |
| 12361396 | 15 | Imidazole inhibitors of cytokine release: probing substituents in the 2 position. |
J Med Chem 45: 4695-705 (2002) | Eberhard-Karls-University Tübingen | 2D 3D TSV |
| 12361393 | 24 | Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase. |
J Med Chem 45: 4669-78 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12361392 | 62 | Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors. |
J Med Chem 45: 4655-68 (2002) | Universit£ degli Studi di Sassari | 2D 3D TSV |
| 12361388 | 47 | Cyclosporins: structure-activity relationships for the inhibition of the human FPR1 formylpeptide receptor. |
J Med Chem 45: 4613-28 (2002) | Strasbourg 1 University | 2D 3D TSV |
| 12361387 | 59 | Cyclosporins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC transporter. |
J Med Chem 45: 4598-612 (2002) | Strasbourg 1 University | 2D 3D TSV |
| 12361386 | 113 | Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. |
J Med Chem 45: 4594-7 (2002) | Friedrich-Alexander University | 2D 3D TSV |
| 12361385 | 34 | Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist. |
J Med Chem 45: 4589-93 (2002) | Merck & Co. | 2D 3D TSV |
| 12358520 | 27 | Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. |
J Am Chem Soc 124: 11852-3 (2002) | Millennium Pharmaceuticals | 2D 3D TSV |
| 12270195 | 15 | Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters. |
Bioorg Med Chem Lett 12: 3009-13 (2002) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12270193 | 23 | 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. |
Bioorg Med Chem Lett 12: 3001-4 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12270192 | 15 | 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity. |
Bioorg Med Chem Lett 12: 2997-3000 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12270191 | 36 | General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain. |
Bioorg Med Chem Lett 12: 2993-6 (2002) | University of California | 2D 3D TSV |
| 12270190 | 18 | Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors. |
Bioorg Med Chem Lett 12: 2989-92 (2002) | Wyeth Research | 2D 3D TSV |
| 12270187 | 12 | Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists. |
Bioorg Med Chem Lett 12: 2977-80 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12270186 | 99 | Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization. |
Bioorg Med Chem Lett 12: 2973-5 (2002) | Idun Pharmaceuticals, Inc. | 2D 3D TSV |
| 12270185 | 257 | Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization. |
Bioorg Med Chem Lett 12: 2969-71 (2002) | Idun Pharmaceuticals, Inc. | 2D 3D TSV |
| 12270184 | 34 | Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines. |
Bioorg Med Chem Lett 12: 2963-7 (2002) | Wyeth Research | 2D 3D TSV |
| 12270183 | 45 | Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines. |
Bioorg Med Chem Lett 12: 2957-61 (2002) | Wyeth Research | 2D 3D TSV |
| 12270180 | 2 | Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor. |
Bioorg Med Chem Lett 12: 2945-8 (2002) | Menarini Ricerche S.p.A. | 2D 3D TSV |
| 12270178 | 74 | Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor. |
Bioorg Med Chem Lett 12: 2935-9 (2002) | CV Therapeutics | 2D 3D TSV |
| 12270177 | 23 | Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase. |
Bioorg Med Chem Lett 12: 2931-4 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12270176 | 41 | Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates. |
Bioorg Med Chem Lett 12: 2925-30 (2002) | Corvas International Inc | 2D 3D TSV |
| 12270175 | 13 | Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC). |
Bioorg Med Chem Lett 12: 2919-23 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12270174 | 34 | Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores. |
Bioorg Med Chem Lett 12: 2913-7 (2002) | Genentech | 2D 3D TSV |
| 12270173 | 23 | Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones. |
Bioorg Med Chem Lett 12: 2907-11 (2002) | Universit£ de Montr£al | 2D 3D TSV |
| 12270171 | 14 | Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents. |
Bioorg Med Chem Lett 12: 2893-7 (2002) | Wyeth Research | 2D 3D TSV |
| 12270170 | 42 | Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors. |
Bioorg Med Chem Lett 12: 2887-91 (2002) | Celera | 2D 3D TSV |
| 12270169 | 13 | Albumin affinity tags increase peptide half-life in vivo. |
Bioorg Med Chem Lett 12: 2883-6 (2002) | Genentech | 2D 3D TSV |
| 12270168 | 40 | Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase. |
Bioorg Med Chem Lett 12: 2879-82 (2002) | Bristol-Myers Squibb PRI | 2D 3D TSV |
| 12270167 | 43 | Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators. |
Bioorg Med Chem Lett 12: 2875-8 (2002) | Bayer Research Center | 2D 3D TSV |
| 12270166 | 8 | Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine. |
Bioorg Med Chem Lett 12: 2871-3 (2002) | Kyorin Pharmaceutical Company Ltd | 2D 3D TSV |
| 12270165 | 80 | Benzodiazepine inhibitors of the MMPs and TACE. |
Bioorg Med Chem Lett 12: 2867-70 (2002) | Wyeth Research | 2D 3D TSV |
| 12270163 | 5 | Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition. |
Bioorg Med Chem Lett 12: 2859-61 (2002) | UPRES EA 1085 | 2D 3D TSV |
| 12270162 | 4 | Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'. |
Bioorg Med Chem Lett 12: 2855-8 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12270156 | 8 | Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a. |
Bioorg Med Chem Lett 12: 2829-31 (2002) | Cephalon Inc | 2D 3D TSV |
| 12270155 | 56 | Development of potent and selective dipeptidyl peptidase II inhibitors. |
Bioorg Med Chem Lett 12: 2825-8 (2002) | University of Antwerp (UIA) | 2D 3D TSV |
| 12270152 | 24 | Convenient synthesis and evaluation of enzyme inhibitory activity of several N-alkyl-, N-phenylalkyl, and cyclic isourea derivatives of 5a-carba-alpha-DL-fucopyranosylamine. |
Bioorg Med Chem Lett 12: 2811-4 (2002) | Keio University | 2D 3D TSV |
| 12244092 | 12 | Structural basis for Chk1 inhibition by UCN-01. |
J Biol Chem 277: 46609-15 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12240953 | 8 | Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2). |
Pharm Res 19: 1244-7 (2002) | University of California | 2D 3D TSV |
| 12238937 | 13 | Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors. |
J Med Chem 45: 4581-4 (2002) | University of Kuopio | 2D 3D TSV |
| 12238936 | 17 | Synthesis of novel 4,1-benzoxazepine derivatives as squalene synthase inhibitors and their inhibition of cholesterol synthesis. |
J Med Chem 45: 4571-80 (2002) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
| 12238935 | 1 | 4-Substituted D-glutamic acid analogues: the first potent inhibitors of glutamate racemase (MurI) enzyme with antibacterial activity. |
J Med Chem 45: 4559-70 (2002) | Eli Lilly and Company | 2D 3D TSV |
| 12238932 | 5 | Inactivation and inhibition of gamma-aminobutyric acid aminotransferase by conformationally restricted vigabatrin analogues. |
J Med Chem 45: 4531-9 (2002) | Northwestern University | 2D 3D TSV |
| 12238930 | 94 | Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. |
J Med Chem 45: 4513-23 (2002) | Kyowa Hakko Kogyo Co., Ltd | 2D 3D TSV |
| 12238929 | 2 | Enhancement of nucleoside cytotoxicity through nucleotide prodrugs. |
J Med Chem 45: 4505-12 (2002) | Southern Research Institute | 2D 3D TSV |
| 12238926 | 99 | Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. |
J Med Chem 45: 4471-84 (2002) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
| 12238924 | 145 | Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B. |
J Med Chem 45: 4443-59 (2002) | Novo Nordisk A/S | 2D 3D TSV |
| 12238922 | 28 | Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics. |
J Med Chem 45: 4419-32 (2002) | Research and Development | 2D 3D TSV |
| 12238919 | 19 | A sorbitol dehydrogenase inhibitor of exceptional in vivo potency with a long duration of action: 1-(R)-[4-[4-(4,6-dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl]ethanol. |
J Med Chem 45: 4398-401 (2002) | Pfizer Inc | 2D 3D TSV |
| 12238918 | 22 | N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine. |
J Med Chem 45: 4395-7 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12238917 | 5 | A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge. |
J Med Chem 45: 4391-4 (2002) | University of Naples Federico II | 2D 3D TSV |
| 12238915 | 18 | Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. |
J Med Chem 45: 4383-6 (2002) | Eli Lilly and Company | 2D 3D TSV |
| 12238914 | 48 | 6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists. |
J Med Chem 45: 4379-82 (2002) | Women's Health Research Institute | 2D 3D TSV |
| 12237342 | 2 | High affinity antagonists of the vanilloid receptor. |
Mol Pharmacol 62: 947-56 (2002) | National Cancer Institute-Bethesda | 2D 3D TSV |
| 12237339 | 2 | Identification of a mechanism by which the methylmercury antidotes N-acetylcysteine and dimercaptopropanesulfonate enhance urinary metal excretion: transport by the renal organic anion transporter-1. |
Mol Pharmacol 62: 921-6 (2002) | University of Rochester School of Medicine | 2D 3D TSV |
| 12235267 | 37 | Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. |
J Pharmacol Exp Ther 303: 323-32 (2002) | St. Jude Children's Research Hospital | 2D 3D TSV |
| 12235265 | 1 | Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate. |
J Pharmacol Exp Ther 303: 308-13 (2002) | AvMax Inc. | 2D 3D TSV |
| 12235229 | 26 | Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. |
J Pharmacol Exp Ther 303: 29-35 (2002) | University of Arkansas | 2D 3D TSV |
| 12232544 | 79 | [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine]. |
Encephale 28: 350-5 (2002) | Emory University | 2D 3D TSV |
| 12223444 | 6 | A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity. |
FASEB J 16: 1829-31 (2002) | CHUL | 2D 3D TSV |
| 12217375 | 6 | Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands. |
Bioorg Med Chem Lett 12: 2781-4 (2002) | National Institutes of Health | 2D 3D TSV |
| 12217372 | 23 | Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors. |
Bioorg Med Chem Lett 12: 2767-70 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12217371 | 12 | 8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors. |
Bioorg Med Chem Lett 12: 2761-5 (2002) | Wyeth-Ayerst Research | 2D 3D TSV |
| 12217369 | 16 | Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors. |
Bioorg Med Chem Lett 12: 2753-6 (2002) | University of Alberta | 2D 3D TSV |
| 12217362 | 10 | Spirocyclic NK(1) antagonists II: [4.5]-spiroethers. |
Bioorg Med Chem Lett 12: 2719-22 (2002) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
| 12217360 | 27 | Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains. |
Bioorg Med Chem Lett 12: 2711-4 (2002) | Mogam Biotechnology Research Institute | 2D 3D TSV |
| 12217358 | 31 | Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 2: substitution of the glycine part. |
Bioorg Med Chem Lett 12: 2703-5 (2002) | University of Antwerp (UIA) | 2D 3D TSV |
| 12217356 | 6 | Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
Bioorg Med Chem Lett 12: 2695-8 (2002) | Ghent University | 2D 3D TSV |
| 12217355 | 39 | Analogue based design of MMP-13 (Collagenase-3) inhibitors. |
Bioorg Med Chem Lett 12: 2689-93 (2002) | GVK Biosciences Pvt. Ltd | 2D 3D TSV |
| 12217351 | 135 | Protease inhibitors: synthesis of matrix metalloproteinase and bacterial collagenase inhibitors incorporating 5-amino-2-mercapto-1,3,4-thiadiazole zinc binding functions. |
Bioorg Med Chem Lett 12: 2667-72 (2002) | Universita degli Studi di Firenze | 2D 3D TSV |
| 12213078 | 31 | Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter. |
J Med Chem 45: 4371-4 (2002) | NIDDK | 2D 3D TSV |
| 12213077 | 18 | Inhibition of the antibacterial target UDP-(3-O-acyl)-N-acetylglucosamine deacetylase (LpxC): isoxazoline zinc amidase inhibitors bearing diverse metal binding groups. |
J Med Chem 45: 4359-70 (2002) | Duke University | 2D 3D TSV |
| 12213075 | 70 | Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). |
J Med Chem 45: 4344-9 (2002) | Purdue University | 2D 3D TSV |
| 12213072 | 29 | 2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. |
J Med Chem 45: 4310-20 (2002) | Novartis Research Institute Vienna | 2D 3D TSV |
| 12213069 | 33 | Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR). |
J Med Chem 45: 4276-81 (2002) | Universita' degli Studi di Siena | 2D 3D TSV |
| 12213067 | 10 | N-[(2-Sulfo)-9-fluorenylmethoxycarbonyl](3)-gentamicin C(1) is a long-acting prodrug derivative. |
J Med Chem 45: 4264-70 (2002) | Institute of Science | 2D 3D TSV |
| 12213066 | 41 | Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase. |
J Med Chem 45: 4254-63 (2002) | Instituto de Qu£mica M£dica (CSIC) | 2D 3D TSV |
| 12213064 | 33 | Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid. |
J Med Chem 45: 4240-5 (2002) | The Royal Danish School of Pharmacy | 2D 3D TSV |
| 12213063 | 4 | Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists. |
J Med Chem 45: 4222-39 (2002) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
| 12213062 | 70 | Synthesis of a novel series of benzocycloalkene derivatives as melatonin receptor agonists. |
J Med Chem 45: 4212-21 (2002) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
| 12213061 | 23 | Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. |
J Med Chem 45: 4202-11 (2002) | University of Gda£?sk | 2D 3D TSV |
| 12213059 | 26 | 6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells. |
J Med Chem 45: 4171-87 (2002) | Novo Nordisk Research and Development | 2D 3D TSV |
| 12213058 | 68 | DrugScore meets CoMFA: adaptation of fields for molecular comparison (AFMoC) or how to tailor knowledge-based pair-potentials to a particular protein. |
J Med Chem 45: 4153-70 (2002) | Philipps-Universit£t Marburg | 2D 3D TSV |
| 12213056 | 42 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
J Med Chem 45: 4128-39 (2002) | Universidad de Navarra | 2D 3D TSV |
| 12213055 | 71 | Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter. |
J Med Chem 45: 4119-27 (2002) | National Institute on Drug Abuse-Intramural Research Program/NIH | 2D 3D TSV |
| 12213054 | 38 | Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
J Med Chem 45: 4110-8 (2002) | Drew University | 2D 3D TSV |
| 12213053 | 117 | Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. |
J Med Chem 45: 4097-109 (2002) | Drew University | 2D 3D TSV |
| 12213052 | 15 | Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction. |
J Med Chem 45: 4094-6 (2002) | Johnson & Johnson Pharmaceutical Research & Development | 2D 3D TSV |
| 12213051 | 207 | Purine and pyrimidine (P2) receptors as drug targets. |
J Med Chem 45: 4057-93 (2002) | National Institute of Diabetes | 2D 3D TSV |
| 12210991 | 24 | Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. |
Chembiochem 3: 897-901 (2002) | New York University | 2D 3D TSV |
| 12206858 | 11 | SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. |
Eur J Pharmacol 450: 191-202 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12204688 | 18 | A quick diversity-oriented amide-forming reaction to optimize P-subsite residues of HIV protease inhibitors. |
Chem Biol 9: 891-6 (2002) | The Scripps Research Institute | 2D 3D TSV |
| 12196020 | 3 | X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement. |
Biochemistry 41: 10810-8 (2002) | Weizmann Institute of Science | 2D 3D TSV |
| 12193020 | 9 | New flavonol oligoglycosides and polyacylated sucroses with inhibitory effects on aldose reductase and platelet aggregation from the flowers of Prunus mume. |
J Nat Prod 65: 1151-5 (2002) | Kyoto Pharmaceutical University | 2D 3D TSV |
| 12193019 | 2 | Naturally occurring cembranes from an Australian sarcophyton species. |
J Nat Prod 65: 1147-50 (2002) | AstraZeneca R&D Griffith University | 2D 3D TSV |
| 12192085 | 52 | Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. |
Proc Natl Acad Sci U S A 99: 11934-9 (2002) | Case Western Reserve University | 2D 3D TSV |
| 12190326 | 11 | Conformationally constrained nicotines: polycyclic, bridged, and spiro-annulated analogues as novel ligands for the nicotinic acetylcholine receptor. |
J Med Chem 45: 4047-54 (2002) | Vienna University of Technology | 2D 3D TSV |
| 12190325 | 13 | Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation. |
J Med Chem 45: 4038-46 (2002) | Columbia University | 2D 3D TSV |
| 12190324 | 15 | Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter. |
J Med Chem 45: 4029-37 (2002) | Research Triangle Institute | 2D 3D TSV |
| 12190321 | 55 | Influence of bulky substituents on histamine h(3) receptor agonist/antagonist properties. |
J Med Chem 45: 4000-10 (2002) | Freie Universit£t Berlin | 2D 3D TSV |
| 12190319 | 15 | Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity. |
J Med Chem 45: 3972-83 (2002) | AstraZeneca Pharmaceuticals LP | 2D 3D TSV |
| 12190316 | 15 | Divalent and trivalent alpha-ketocarboxylic acids as inhibitors of protein tyrosine phosphatases. |
J Med Chem 45: 3946-52 (2002) | Brown University | 2D 3D TSV |
| 12190315 | 43 | Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach. |
J Med Chem 45: 3934-45 (2002) | Instituto de Qu£mica M£dica (CSIC) | 2D 3D TSV |
| 12190314 | 15 | Synthesis and evaluation of Glypsi(PO(2)R-N)Pro-containing pseudopeptides as novel inhibitors of the human cyclophilin hCyp-18. |
J Med Chem 45: 3928-33 (2002) | Departement D'Ingenierie et D'Etudes des Proteines | 2D 3D TSV |
| 12190313 | 94 | Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. |
J Med Chem 45: 3905-27 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12190312 | 67 | Chiral N,N-disubstituted trifluoro-3-amino-2-propanols are potent inhibitors of cholesteryl ester transfer protein. |
J Med Chem 45: 3891-904 (2002) | Pharmacia | 2D 3D TSV |
| 12190311 | 37 | Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151). |
J Med Chem 45: 3878-90 (2002) | GSK | 2D 3D TSV |
| 12190310 | 27 | Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography. |
J Med Chem 45: 3865-77 (2002) | Pfizer Inc | 2D 3D TSV |
| 12190309 | 14 | Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase. |
J Med Chem 45: 3854-64 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12190308 | 36 | Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers. |
J Med Chem 45: 3844-53 (2002) | University of Bologna | 2D 3D TSV |
| 12190306 | 14 | Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
J Med Chem 45: 3829-35 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12190304 | 10 | Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors. |
J Med Chem 45: 3820-3 (2002) | University of Maryland | 2D 3D TSV |
| 12190302 | 9 | Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. |
J Med Chem 45: 3813-5 (2002) | Biovitrum | 2D 3D TSV |
| 12183686 | 38 | Effects of pyridine ring substitutions on affinity, efficacy, and subtype selectivity of neuronal nicotinic receptor agonist epibatidine. |
J Pharmacol Exp Ther 302: 1246-52 (2002) | University of Miami | 2D 3D TSV |
| 12182878 | 12 | The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors. |
Bioorg Med Chem Lett 12: 2643-6 (2002) | The Schering Plough Research Institute | 2D 3D TSV |
| 12182871 | 3 | Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure. |
Bioorg Med Chem Lett 12: 2607-9 (2002) | Universidade de Vigo | 2D 3D TSV |
| 12182870 | 54 | The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man. |
Bioorg Med Chem Lett 12: 2603-6 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12182866 | 83 | 8-Aryl xanthines potent inhibitors of phosphodiesterase 5. |
Bioorg Med Chem Lett 12: 2587-90 (2002) | Novartis Horsham Research Centre | 2D 3D TSV |
| 12182865 | 88 | Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor. |
Bioorg Med Chem Lett 12: 2583-6 (2002) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12182862 | 56 | Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade. |
Bioorg Med Chem Lett 12: 2569-72 (2002) | Organon Laboratories Ltd | 2D 3D TSV |
| 12182861 | 37 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
Bioorg Med Chem Lett 12: 2565-8 (2002) | Organon Laboratories Ltd | 2D 3D TSV |
| 12182860 | 72 | Dihydroquinolines as novel n-NOS inhibitors. |
Bioorg Med Chem Lett 12: 2561-4 (2002) | Schering AG | 2D 3D TSV |
| 12182858 | 11 | Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group. |
Bioorg Med Chem Lett 12: 2553-6 (2002) | University of Antwerp (UIA) | 2D 3D TSV |
| 12182857 | 5 | Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles: new selective ligands of the 5-HT(7) receptor. |
Bioorg Med Chem Lett 12: 2549-52 (2002) | Meiji Seika Kaisha, Ltd | 2D 3D TSV |
| 12182856 | 18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
Bioorg Med Chem Lett 12: 2545-8 (2002) | AtheroGenics, Inc. | 2D 3D TSV |
| 12182854 | 45 | A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold. |
Bioorg Med Chem Lett 12: 2535-9 (2002) | Universit£ Libre de Bruxelles | 2D 3D TSV |
| 12182851 | 15 | Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands. |
Bioorg Med Chem Lett 12: 2519-22 (2002) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12182850 | 19 | Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals. |
Bioorg Med Chem Lett 12: 2515-8 (2002) | Merck Sharp and Dohme Research Laboratories | 2D 3D TSV |
| 12182847 | 12 | Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe. |
Bioorg Med Chem Lett 12: 2501-5 (2002) | University of Nottingham | 2D 3D TSV |
| 12176106 | 20 | A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. |
Eur J Pharmacol 450: 37-41 (2002) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12176030 | 12 | Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. |
Biochem Biophys Res Commun 296: 644-50 (2002) | Kyushu University | 2D 3D TSV |
| 12166953 | 9 | Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators. |
J Med Chem 45: 3809-12 (2002) | University of Bonn | 2D 3D TSV |
| 12166952 | 6 | Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide. |
J Med Chem 45: 3805-8 (2002) | Otsuka Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12166951 | 146 | Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists. |
J Med Chem 45: 3794-804 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12166950 | 208 | Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
J Med Chem 45: 3772-93 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12166948 | 77 | Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. |
J Med Chem 45: 3755-64 (2002) | Boehringer Ingelheim Pharma KG | 2D 3D TSV |
| 12166947 | 30 | Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands. |
J Med Chem 45: 3746-54 (2002) | University of California | 2D 3D TSV |
| 12166946 | 28 | N-Acylvanillamides: development of an expeditious synthesis and discovery of new acyl templates for powerful activation of the vanilloid receptor. |
J Med Chem 45: 3739-45 (2002) | Istituto per la Chimica di Molecole di Interesse Biologico | 2D 3D TSV |
| 12166944 | 48 | Oxygenated metabolites of anandamide and 2-arachidonoylglycerol: conformational analysis and interaction with cannabinoid receptors, membrane transporter, and fatty acid amide hydrolase. |
J Med Chem 45: 3709-20 (2002) | Utrecht University | 2D 3D TSV |
| 12166943 | 81 | 1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
J Med Chem 45: 3703-8 (2002) | Nutrition Research Institute | 2D 3D TSV |
| 12166942 | 4 | The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. |
J Med Chem 45: 3692-702 (2002) | The Institute of Cancer Research | 2D 3D TSV |
| 12166941 | 42 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
J Med Chem 45: 3684-91 (2002) | National Institutes of Health | 2D 3D TSV |
| 12166939 | 6 | (+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist. |
J Med Chem 45: 3660-8 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12166938 | 8 | Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor. |
J Med Chem 45: 3649-59 (2002) | Kennesaw State University | 2D 3D TSV |
| 12166937 | 26 | Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors. |
J Med Chem 45: 3639-48 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12166933 | 24 | Alpha(1)-adrenoceptor antagonists. 4. Pharmacophore-based design, synthesis, and biological evaluation of new imidazo-, benzimidazo-, and indoloarylpiperazine derivatives. |
J Med Chem 45: 3603-11 (2002) | Università di Pisa | 2D 3D TSV |
| 12166932 | 14 | Successful virtual screening for novel inhibitors of human carbonic anhydrase: strategy and experimental confirmation. |
J Med Chem 45: 3588-602 (2002) | University of Marburg | 2D 3D TSV |
| 12166931 | 13 | Nonaromatic sulfonamide group as an ideal anchor for potent human carbonic anhydrase inhibitors: role of hydrogen-bonding networks in ligand binding and drug design. |
J Med Chem 45: 3583-7 (2002) | Universit£ degli Studi di Firenze | 2D 3D TSV |
| 12166930 | 21 | Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist. |
J Med Chem 45: 3579-82 (2002) | TBA | 2D 3D TSV |
| 12166927 | 6 | 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. |
J Med Chem 45: 3569-72 (2002) | TBA | 2D 3D TSV |
| 12161164 | 14 | Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase. |
Bioorg Med Chem Lett 12: 2487-90 (2002) | National Institute of Diabetes and Digestive and Kidney Diseases | 2D 3D TSV |
| 12161162 | 69 | N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Bioorg Med Chem Lett 12: 2479-82 (2002) | Hoffmann-La Roche Inc | 2D 3D TSV |
| 12161161 | 94 | N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Bioorg Med Chem Lett 12: 2475-8 (2002) | Roche Research Center | 2D 3D TSV |
| 12161160 | 15 | Investigation of the PDZ domain ligand binding site using chemically modified peptides. |
Bioorg Med Chem Lett 12: 2471-4 (2002) | University of California | 2D 3D TSV |
| 12161158 | 11 | Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics. |
Bioorg Med Chem Lett 12: 2463-5 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12161155 | 33 | 1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT(7) receptor ligands. |
Bioorg Med Chem Lett 12: 2451-4 (2002) | NPS Pharmaceuticals Inc | 2D 3D TSV |
| 12161154 | 11 | An improved synthesis of the C-linked glucuronide of N-(4-hydroxyphenyl)retinamide. |
Bioorg Med Chem Lett 12: 2447-50 (2002) | The Ohio State University | 2D 3D TSV |
| 12161153 | 39 | Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists. |
Bioorg Med Chem Lett 12: 2443-6 (2002) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12161148 | 17 | Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains. |
Bioorg Med Chem Lett 12: 2423-6 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12161147 | 5 | Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains. |
Bioorg Med Chem Lett 12: 2419-22 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12161144 | 23 | Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution. |
Bioorg Med Chem Lett 12: 2407-10 (2002) | Roche Research Center | 2D 3D TSV |
| 12161142 | 34 | C-3 Amido-indole cannabinoid receptor modulators. |
Bioorg Med Chem Lett 12: 2399-402 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12161140 | 12 | Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. |
Bioorg Med Chem Lett 12: 2391-4 (2002) | Kingston University | 2D 3D TSV |
| 12161139 | 11 | Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes. |
Bioorg Med Chem Lett 12: 2387-90 (2002) | University of New Orleans | 2D 3D TSV |
| 12161137 | 39 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
Bioorg Med Chem Lett 12: 2377-80 (2002) | Friedrich-Alexander University | 2D 3D TSV |
| 12161135 | 17 | Novel inhibitors of plasminogen activator inhibitor-1: development of new templates from diketopiperazines. |
Bioorg Med Chem Lett 12: 2367-70 (2002) | Xenova Ltd. | 2D 3D TSV |
| 12161132 | 102 | Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity. |
Bioorg Med Chem Lett 12: 2355-8 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12161131 | 1 | Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry. |
Bioorg Med Chem Lett 12: 2349-53 (2002) | Minase Research Institute | 2D 3D TSV |
| 12161128 | 35 | Synthesis of [(2S,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]-5-methylfuran-4-carboxylic acid derivatives: new leads as selective beta-galactosidase inhibitors. |
Bioorg Med Chem Lett 12: 2335-9 (2002) | Universidad de Sevilla | 2D 3D TSV |
| 12161123 | 13 | A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. |
Bioorg Med Chem Lett 12: 2313-6 (2002) | Korea Institute of Science & Technology | 2D 3D TSV |
| 12161118 | 28 | Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines. |
Bioorg Med Chem Lett 12: 2291-4 (2002) | Fukui Research Institute | 2D 3D TSV |
| 12161117 | 2 | 3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists. |
Bioorg Med Chem Lett 12: 2287-90 (2002) | Chinese Academy of Sciences | 2D 3D TSV |
| 12161114 | 64 | 3D-QSAR studies on 4-hydroxyphenylpyruvate dioxygenase inhibitors by comparative molecular field analysis (CoMFA). |
Bioorg Med Chem Lett 12: 2271-5 (2002) | Zhejiang University | 2D 3D TSV |
| 12161113 | 8 | L-Cysteine based N-type calcium channel blockers: structure-activity relationships of the C-terminal lipophilic moiety, and oral analgesic efficacy in rat pain models. |
Bioorg Med Chem Lett 12: 2267-9 (2002) | Minase Research Institute | 2D 3D TSV |
| 12161112 | 14 | Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor. |
Bioorg Med Chem Lett 12: 2263-6 (2002) | Universita' di Firenze | 2D 3D TSV |
| 12144928 | 11 | Sequencing, modeling, and selective inhibition of Trypanosoma brucei hexokinase. |
Chem Biol 9: 839-47 (2002) | Universite Paul Sabatier | 2D 3D TSV |
| 12141869 | 2 | Agonodepsides a and B: two new depsides from a filamentous fungus F7524. |
J Nat Prod 65: 1037-8 (2002) | Institute of Molecular and Cell Biology | 2D 3D TSV |
| 12141863 | 1 | Bioactive abietane and seco-abietane diterpenoids from Salvia prionitis. |
J Nat Prod 65: 1016-20 (2002) | Chinese Academy of Sciences | 2D 3D TSV |
| 12139467 | 17 | Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. |
J Med Chem 45: 3558-68 (2002) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12139466 | 11 | Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
J Med Chem 45: 3549-57 (2002) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12139463 | 24 | Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans. |
J Med Chem 45: 3524-30 (2002) | Research Triangle Institute | 2D 3D TSV |
| 12139462 | 34 | Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity. |
J Med Chem 45: 3509-23 (2002) | AstraZeneca | 2D 3D TSV |
| 12139459 | 74 | Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid. |
J Med Chem 45: 3482-90 (2002) | Pfizer Inc | 2D 3D TSV |
| 12139455 | 78 | Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents. |
J Med Chem 45: 3451-7 (2002) | Genentech Inc | 2D 3D TSV |
| 12139454 | 56 | Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists. |
J Med Chem 45: 3440-50 (2002) | University of Bonn | 2D 3D TSV |
| 12139452 | 29 | Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies. |
J Med Chem 45: 3418-29 (2002) | Menarini Ricerche S.p.A. | 2D 3D TSV |
| 12139451 | 41 | Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors. |
J Med Chem 45: 3406-17 (2002) | Saarland University | 2D 3D TSV |
| 12139450 | 29 | Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase. |
J Med Chem 45: 3394-405 (2002) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
| 12139449 | 114 | Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. |
J Med Chem 45: 3381-93 (2002) | University of Newcastle | 2D 3D TSV |
| 12139447 | 6 | (4R,5S)/(4S,5R)-4,5-Bis(4-hydroxyphenyl)-2-imidazolines: ligands for the estrogen receptor with a novel binding mode. |
J Med Chem 45: 3356-65 (2002) | Free University of Berlin | 2D 3D TSV |
| 12139445 | 36 | Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. |
J Med Chem 45: 3337-44 (2002) | Instituto de Química Médica (CSIC) | 2D 3D TSV |
| 12134946 | 6 | Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? |
Pharm Res 19: 773-9 (2002) | The University of Kansas | 2D 3D TSV |
| 12134945 | 9 | Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? |
Pharm Res 19: 765-72 (2002) | The University of Kansas | 2D 3D TSV |
| 12130738 | 11 | SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. |
J Pharmacol Exp Ther 302: 731-41 (2002) | Sanofi-Synthelabo Recherche | 2D 3D TSV |
| 12130733 | 17 | Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors. |
J Pharmacol Exp Ther 302: 687-95 (2002) | University of Kentucky | 2D 3D TSV |
| 12130730 | 8 | Characterization of methotrexate transport and its drug interactions with human organic anion transporters. |
J Pharmacol Exp Ther 302: 666-71 (2002) | Kyorin University | 2D 3D TSV |
| 12130727 | 2 | Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4. |
J Pharmacol Exp Ther 302: 645-50 (2002) | Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology | 2D 3D TSV |
| 12128170 | 10 | Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression. |
Eur J Pharm Sci 16: 159-65 (2002) | Kyoto Pharmaceutical University | 2D 3D TSV |
| 12127545 | 4 | Binding modes of two novel dinucleotide inhibitors of HIV-1 integrase. |
Bioorg Med Chem Lett 12: 2233-6 (2002) | The University of Iowa | 2D 3D TSV |
| 12127543 | 26 | Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines. |
Bioorg Med Chem Lett 12: 2225-8 (2002) | Southern Research Institute | 2D 3D TSV |
| 12127538 | 26 | N-aryl-prolyl-dipeptides as potent antagonists of VLA-4. |
Bioorg Med Chem Lett 12: 2205-8 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12127537 | 16 | Design and synthesis of novel inhibitors of gelatinase B. |
Bioorg Med Chem Lett 12: 2201-4 (2002) | University of California | 2D 3D TSV |
| 12127536 | 22 | Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis. |
Bioorg Med Chem Lett 12: 2197-200 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12127534 | 8 | Phosphonate and phosphinate analogues of N-acylated gamma-glutamylglutamate. potent inhibitors of glutamate carboxypeptidase II. |
Bioorg Med Chem Lett 12: 2189-92 (2002) | Guilford Pharmaceuticals Inc | 2D 3D TSV |
| 12127533 | 23 | Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. |
Bioorg Med Chem Lett 12: 2185-7 (2002) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12127532 | 22 | Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. |
Bioorg Med Chem Lett 12: 2179-83 (2002) | Neurocrine Biosciences Inc | 2D 3D TSV |
| 12127526 | 75 | Rational design of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2(p185(erbB)) tyrosine kinases. |
Bioorg Med Chem Lett 12: 2153-7 (2002) | SUGEN, Inc. | 2D 3D TSV |
| 12127524 | 39 | Novel thiophene derivatives for the treatment of benign prostatic hyperplasia. |
Bioorg Med Chem Lett 12: 2145-8 (2002) | Johnson & Johnson Pharmaceutical Research and Development LLC | 2D 3D TSV |
| 12127523 | 22 | N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists. |
Bioorg Med Chem Lett 12: 2141-4 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12127522 | 30 | Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase. |
Bioorg Med Chem Lett 12: 2137-40 (2002) | Bristol-Myers Squibb Pharmaceutical Research Institute | 2D 3D TSV |
| 12127521 | 33 | 3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists. |
Bioorg Med Chem Lett 12: 2133-6 (2002) | Neurogen Corporation | 2D 3D TSV |
| 12127519 | 40 | Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist. |
Bioorg Med Chem Lett 12: 2125-8 (2002) | The Schering Plough Research Institute | 2D 3D TSV |
| 12127518 | 23 | The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class. |
Bioorg Med Chem Lett 12: 2121-3 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12127516 | 41 | Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5. |
Bioorg Med Chem Lett 12: 2113-6 (2002) | Abbott GmbH & Co. KG | 2D 3D TSV |
| 12127515 | 29 | SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors. |
Bioorg Med Chem Lett 12: 2109-12 (2002) | Novartis Pharma AG | 2D 3D TSV |
| 12127511 | 13 | 4,4'-Benzophenone-O,O'-disulfamate: a potent inhibitor of steroid sulfatase. |
Bioorg Med Chem Lett 12: 2093-5 (2002) | Novartis Research Institute Vienna | 2D 3D TSV |
| 12127510 | 2 | Essential structural factors of acetogenins, potent inhibitors of mitochondrial complex I. |
Bioorg Med Chem Lett 12: 2089-92 (2002) | Kyoto University | 2D 3D TSV |
| 12127507 | 11 | A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones. |
Bioorg Med Chem Lett 12: 2073-7 (2002) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
| 12127505 | 28 | Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists. |
Bioorg Med Chem Lett 12: 2065-8 (2002) | Novartis Pharma AG | 2D 3D TSV |
| 12113838 | 36 | Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification. |
Bioorg Med Chem Lett 12: 2043-6 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12113836 | 162 | Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs. |
Bioorg Med Chem Lett 12: 2035-7 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12113835 | 176 | Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1. |
Bioorg Med Chem Lett 12: 2031-4 (2002) | Abbott Laboratories | 2D 3D TSV |
| 12113834 | 64 | The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases. |
Bioorg Med Chem Lett 12: 2027-30 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12113833 | 183 | 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors. |
Bioorg Med Chem Lett 12: 2023-6 (2002) | Celera | 2D 3D TSV |
| 12113832 | 120 | 2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors. |
Bioorg Med Chem Lett 12: 2019-22 (2002) | Celera | 2D 3D TSV |
| 12113830 | 13 | Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles. |
Bioorg Med Chem Lett 12: 2011-4 (2002) | Wyeth Research | 2D 3D TSV |
| 12113828 | 63 | N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities. |
Bioorg Med Chem Lett 12: 2001-5 (2002) | University of Paris | 2D 3D TSV |
| 12113827 | 7 | Translocation of the 5-alkoxy substituent of 2,5-dialkoxyarylalkylamines to the 6-position: effects on 5-HT(2A/2C) receptor affinity. |
Bioorg Med Chem Lett 12: 1997-9 (2002) | Purdue University | 2D 3D TSV |
| 12113826 | 23 | Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy. |
Bioorg Med Chem Lett 12: 1993-6 (2002) | University of Illinois at Chicago | 2D 3D TSV |
| 12113820 | 4 | Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects. |
Bioorg Med Chem Lett 12: 1967-71 (2002) | Wyeth Research | 2D 3D TSV |
| 12113816 | 7 | The synthesis and effect of fluorinated chalcone derivatives on nitric oxide production. |
Bioorg Med Chem Lett 12: 1951-4 (2002) | Universidad de Valencia | 2D 3D TSV |
| 12113814 | 60 | Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents. |
Bioorg Med Chem Lett 12: 1941-6 (2002) | Korea Research Institute of Chemical Technology | 2D 3D TSV |
| 12113813 | 53 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
Bioorg Med Chem Lett 12: 1937-40 (2002) | Friedrich-Alexander University | 2D 3D TSV |
| 12113810 | 20 | Synthesis and anti-influenza virus activity of 7-O-alkylated derivatives related to zanamivir. |
Bioorg Med Chem Lett 12: 1925-8 (2002) | Sankyo Co., Ltd | 2D 3D TSV |
| 12113809 | 12 | Synthesis and anti-influenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives. |
Bioorg Med Chem Lett 12: 1921-4 (2002) | Sankyo Co., Ltd | 2D 3D TSV |
| 12113806 | 40 | Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists. |
Bioorg Med Chem Lett 12: 1909-12 (2002) | Ghent University | 2D 3D TSV |
| 12110997 | 380 | In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs. |
Psychopharmacology (Berl) 162: 193-202 (2002) | Westfälische Wilhelms-Universitä Muenster, | 2D 3D TSV |
| 12110607 | 24 | Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. |
Br J Pharmacol 136: 829-36 (2002) | University of Bonn | 2D 3D TSV |
| 12109915 | 5 | Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres. |
J Med Chem 45: 3321-4 (2002) | University of the Mediterranean | 2D 3D TSV |
| 12109914 | 24 | Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment. |
J Med Chem 45: 3310-20 (2002) | University of California | 2D 3D TSV |
| 12109913 | 25 | Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells. |
J Med Chem 45: 3296-309 (2002) | Westfälische Wilhelms-Universität Münster | 2D 3D TSV |
| 12109912 | 9 | Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure. |
J Med Chem 45: 3286-95 (2002) | University of Bologna | 2D 3D TSV |
| 12109911 | 47 | Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine. |
J Med Chem 45: 3280-5 (2002) | University Center for Pharmacy | 2D 3D TSV |
| 12109910 | 8 | N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands. |
J Med Chem 45: 3271-9 (2002) | Universit£ di Camerino | 2D 3D TSV |
| 12109908 | 29 | Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI). |
J Med Chem 45: 3246-56 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12109907 | 8 | Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. |
J Med Chem 45: 3235-45 (2002) | University of Bath | 2D 3D TSV |
| 12109906 | 9 | Structure-based approach for binding site identification on AmpC beta-lactamase. |
J Med Chem 45: 3222-34 (2002) | Northwestern University | 2D 3D TSV |
| 12109905 | 54 | 4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor. |
J Med Chem 45: 3210-21 (2002) | University of Chicago Medical Center | 2D 3D TSV |
| 12109903 | 50 | Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors. |
J Med Chem 45: 3184-94 (2002) | National Cancer Institute/NIH | 2D 3D TSV |
| 12109902 | 15 | Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity. |
J Med Chem 45: 3171-83 (2002) | Parc Club Orsay Universit£ | 2D 3D TSV |
| 12109901 | 45 | SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement. |
J Med Chem 45: 3161-70 (2002) | Georgetown University Medical Center | 2D 3D TSV |
| 12106615 | 4 | Inhibition of transport across the hepatocyte canalicular membrane by the antibiotic fusidate. |
Biochem Pharmacol 64: 151-8 (2002) | Deutsches Krebsforschungszentrum | 2D 3D TSV |
| 12093278 | 30 | Amplification of the effects of drug resistance mutations by background polymorphisms in HIV-1 protease from African subtypes. |
Biochemistry 41: 8613-9 (2002) | The Johns Hopkins University | 2D 3D TSV |
| 12089149 | 1 | Molecular identification of a novel carnitine transporter specific to human testis. Insights into the mechanism of carnitine recognition. |
J Biol Chem 277: 36262-71 (2002) | Kyorin University | 2D 3D TSV |
| 12088440 | 3 | Callyspongynic acid, a polyacetylenic acid which inhibits alpha-glucosidase, from the marine sponge Callyspongia truncata. |
J Nat Prod 65: 922-4 (2002) | The University of Tokyo | 2D 3D TSV |
| 12086500 | 59 | Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity. |
J Med Chem 45: 3143-60 (2002) | Schering-Plough Research Institute | 2D 3D TSV |
| 12086497 | 64 | Potent, novel in vitro inhibitors of the Pseudomonas aeruginosa deacetylase LpxC. |
J Med Chem 45: 3112-29 (2002) | Chiron Corporation | 2D 3D TSV |
| 12086495 | 130 | Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors. |
J Med Chem 45: 3094-102 (2002) | Pfizer Inc. | 2D 3D TSV |
| 12086493 | 120 | Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position. |
J Med Chem 45: 3073-81 (2002) | University of Florida | 2D 3D TSV |
| 12086491 | 116 | Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives. |
J Med Chem 45: 3057-66 (2002) | Pharmaceutical Research Institute | 2D 3D TSV |
| 12086490 | 5 | Modification of the structure of a metallopeptide: synthesis and biological evaluation of (111)In-labeled DOTA-conjugated rhenium-cyclized alpha-MSH analogues. |
J Med Chem 45: 3048-56 (2002) | University of Missouri-Columbia | 2D 3D TSV |
| 12086489 | 19 | Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. |
J Med Chem 45: 3041-7 (2002) | University of New Orleans | 2D 3D TSV |
| 12086487 | 28 | Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety. |
J Med Chem 45: 3022-31 (2002) | University of Groningen | 2D 3D TSV |
| 12086486 | 45 | Novel, non-acylguanidine-type Na(+)/H(+) exchanger inhibitors: synthesis and pharmacology of 5-tetrahydroquinolinylidene aminoguanidine derivatives. |
J Med Chem 45: 3009-21 (2002) | Takeda Chemical Industries, Ltd | 2D 3D TSV |
| 12086485 | 10 | Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
J Med Chem 45: 2994-3008 (2002) | Boehringer Ingelheim Pharmaceuticals Inc | 2D 3D TSV |
| 12086484 | 13 | Identification of potent and novel alpha4beta1 antagonists using in silico screening. |
J Med Chem 45: 2988-93 (2002) | Biogen Inc | 2D 3D TSV |
| 12086480 | 65 | Structural requirements for inhibition of the neuronal nitric oxide synthase (NOS-I): 3D-QSAR analysis of 4-oxo- and 4-amino-pteridine-based inhibitors. |
J Med Chem 45: 2923-41 (2002) | Aventis Pharma | 2D 3D TSV |
| 12086479 | 11 | Principles governing the binding of a class of non-peptidic inhibitors to the SH2 domain of src studied by X-ray analysis. |
J Med Chem 45: 2915-22 (2002) | Aventis Pharma | 2D 3D TSV |
| 12086475 | 1 | Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties. |
J Med Chem 45: 2887-90 (2002) | University of Minnesota | 2D 3D TSV |
| 12085361 | 7 | Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. |
Hepatology 36: 164-72 (2002) | University Hospital | 2D 3D TSV |
| 12067561 | 97 | CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships. |
Bioorg Med Chem Lett 12: 1785-9 (2002) | Bristol-Myers Squibb Co. | 2D 3D TSV |
| 12067559 | 34 | Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol. |
Bioorg Med Chem Lett 12: 1775-8 (2002) | University of Michigan | 2D 3D TSV |
| 12067558 | 15 | High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists. |
Bioorg Med Chem Lett 12: 1771-4 (2002) | Lundbeck Research USA, Inc. | 2D 3D TSV |
| 12067557 | 24 | Discovery of potent and selective small molecule NPY Y5 receptor antagonists. |
Bioorg Med Chem Lett 12: 1767-9 (2002) | Lundbeck Research USA, Inc. | 2D 3D TSV |
| 12067556 | 8 | Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds. |
Bioorg Med Chem Lett 12: 1763-6 (2002) | University College Dublin | 2D 3D TSV |
| 12067555 | 31 | 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II. |
Bioorg Med Chem Lett 12: 1759-62 (2002) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
| 12067554 | 27 | 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I. |
Bioorg Med Chem Lett 12: 1755-8 (2002) | Merck Sharp & Dohme Research Laboratories | 2D 3D TSV |
| 12067551 | 10 | Discovery of imidazole glycerol phosphate dehydratase inhibitors through 3-D database searching. |
Bioorg Med Chem Lett 12: 1743-6 (2002) | Monsanto Company | 2D 3D TSV |
| 12067547 | 16 | Synthesis of triazole-Tethered pyrrolidine libraries: novel ECE inhibitors. |
Bioorg Med Chem Lett 12: 1727-30 (2002) | F. Hoffmann-La Roche Inc | 2D 3D TSV |
| 12067545 | 22 | Pyrrolidine-5,5-trans-lactams as novel mechanism-based inhibitors of human cytomegalovirus protease. Part 3: potency and plasma stability. |
Bioorg Med Chem Lett 12: 1719-22 (2002) | GlaxoSmithKline | 2D 3D TSV |
| 12067543 | 11 | Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase. |
Bioorg Med Chem Lett 12: 1709-13 (2002) | Tunghai University | 2D 3D TSV |
| 12065740 | 8 | 8-Carboxamidocyclazocine: a long-acting, novel benzomorphan. |
J Pharmacol Exp Ther 302: 374-80 (2002) | University of Rochester | 2D 3D TSV |
| 12065738 | 9 | Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties. |
J Pharmacol Exp Ther 302: 359-68 (2002) | Bayer AG | 2D 3D TSV |
| 12065734 | 57 | A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors. |
J Pharmacol Exp Ther 302: 328-36 (2002) | University of North Carolina at Chapel Hill | 2D 3D TSV |
| 12065700 | 14 | Biochemistry and pharmacology of epitope-tagged alpha(1)-adrenergic receptor subtypes. |
J Pharmacol Exp Ther 302: 58-65 (2002) | Emory University | 2D 3D TSV |
| 12065655 | 26 | Pharmacological characterization of cloned chicken neuropeptide Y receptors Y1 and Y5. |
J Neurochem 81: 462-71 (2002) | Uppsala University | 2D 3D TSV |
| 12065583 | 3 | Identification of a novel human eicosanoid receptor coupled to G(i/o). |
J Biol Chem 277: 31459-65 (2002) | Tanabe Seiyaku Co., Ltd | 2D 3D TSV |
| 12063169 | 4 | Role of human organic anion transporter 4 in the transport of ochratoxin A. |
Biochim Biophys Acta 1590: 64-75 (2002) | Kyorin University | 2D 3D TSV |
| 12061890 | 26 | Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors. |
J Med Chem 45: 2877-85 (2002) | MethylGene Inc | 2D 3D TSV |
| 12061886 | 11 | Synthesis and evaluation of a novel series of 2-chloro-5-((1-methyl-2-(S)-pyrrolidinyl)methoxy)-3-(2-(4-pyridinyl)vinyl)pyridine analogues as potential positron emission tomography imaging agents for nicotinic acetylcholine receptors. |
J Med Chem 45: 2841-9 (2002) | National Institute on Drug Abuse | 2D 3D TSV |
| 12061885 | 22 | Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian alpha4beta2 and Drosophila nicotinic receptors. |
J Med Chem 45: 2832-40 (2002) | University of California | 2D 3D TSV |
| 12061882 | 83 | Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position. |
J Med Chem 45: 2801-10 (2002) | University of Florida | 2D 3D TSV |
| 12061881 | 94 | Synthesis and structure-affinity-activity relationships of novel benzofuran derivatives as MT(2) melatonin receptor selective ligands. |
J Med Chem 45: 2788-800 (2002) | Institut de Chimie Pharmaceutique Albert Lespagnol | 2D 3D TSV |
| 12061879 | 44 | SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions. |
J Med Chem 45: 2770-80 (2002) | Harvard University | 2D 3D TSV |
| 12061878 | 100 | Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa. |
J Med Chem 45: 2749-69 (2002) | Aventis Pharma Deutschland GmbH | 2D 3D TSV |
| 12061876 | 53 | From imidazoles to pyrimidines: new inhibitors of cytokine release. |
J Med Chem 45: 2733-40 (2002) | Eberhard-Karls-University T£bingen | 2D 3D TSV |
| 12061874 | 60 | Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB(1) receptor antagonist N-(piperidinyl)- 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716). |
J Med Chem 45: 2708-19 (2002) | Research Triangle Institute | 2D 3D TSV |
| 12061873 | 79 | Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain. |
J Med Chem 45: 2695-707 (2002) | University of California San Francisco | 2D 3D TSV |
| 12057671 | 16 | Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents. |
Bioorg Med Chem 10: 2807-16 (2002) | Purdue University | 2D 3D TSV |
| 12054506 | 26 | The motilin pharmacophore in CHO cells expressing the human motilin receptor. |
Biochem Biophys Res Commun 293: 1223-7 (2002) | Katholieke Universiteit Leuven | 2D 3D TSV |
| 12044152 | 4 | DNA gyrase interaction with coumarin-based inhibitors: the role of the hydroxybenzoate isopentenyl moiety and the 5'-methyl group of the noviose. |
Biochemistry 41: 7217-23 (2002) | UMR CNRS 6032 | 2D 3D TSV |
| 12039591 | 63 | Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight. |
Bioorg Med Chem Lett 12: 1687-90 (2002) | Abbott Bioresearch Center | 2D 3D TSV |
| 12039590 | 51 | Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. |
Bioorg Med Chem Lett 12: 1683-6 (2002) | Abbott Bioresearch Center | 2D 3D TSV |
| 12039589 | 6 | Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists. |
Bioorg Med Chem Lett 12: 1679-82 (2002) | Roche Research Center | 2D 3D TSV |
| 12039587 | 39 | Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity. |
Bioorg Med Chem Lett 12: 1671-4 (2002) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12039586 | 42 | Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency. |
Bioorg Med Chem Lett 12: 1667-70 (2002) | Aventis Pharmaceuticals, Inc. | 2D 3D TSV |
| 12039585 | 52 | Cephalosporin-derived inhibitors of beta-lactamase. Part 4: The C3 substituent. |
Bioorg Med Chem Lett 12: 1663-6 (2002) | Southern Methodist University | 2D 3D TSV |
| 12039584 | 59 | Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors. |
Bioorg Med Chem Lett 12: 1657-61 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12039583 | 140 | Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides. |
Bioorg Med Chem Lett 12: 1651-5 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12039576 | 17 | Synthesis and profile of SCH351591, a novel PDE4 inhibitor. |
Bioorg Med Chem Lett 12: 1621-3 (2002) | Schering-Plough Corporation | 2D 3D TSV |
| 12039575 | 18 | 8-Methoxyquinolines as PDE4 inhibitors. |
Bioorg Med Chem Lett 12: 1617-9 (2002) | Schering-Plough Corporation | 2D 3D TSV |
| 12039574 | 16 | 8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma. |
Bioorg Med Chem Lett 12: 1613-5 (2002) | Celltech R&D Ltd | 2D 3D TSV |
| 12039572 | 7 | Exploration of peptidyl hydrazones as water-soluble calpain inhibitors. |
Bioorg Med Chem Lett 12: 1603-6 (2002) | Senju Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12039571 | 19 | Development of tripeptidyl farnesyltransferase inhibitors. |
Bioorg Med Chem Lett 12: 1599-602 (2002) | Department of Chemistry and School of Molecular Science(BK21) | 2D 3D TSV |
| 12039570 | 51 | N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists. |
Bioorg Med Chem Lett 12: 1595-8 (2002) | Celltech R&D Ltd | 2D 3D TSV |
| 12039569 | 36 | Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists. |
Bioorg Med Chem Lett 12: 1591-4 (2002) | Celltech R&D Ltd | 2D 3D TSV |
| 12039564 | 1 | Solid-phase synthesis of thrombin inhibitors. |
Bioorg Med Chem Lett 12: 1571-3 (2002) | BASF AG | 2D 3D TSV |
| 12039562 | 17 | 2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors. |
Bioorg Med Chem Lett 12: 1563-6 (2002) | University of Virginia | 2D 3D TSV |
| 12039561 | 30 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
Bioorg Med Chem Lett 12: 1559-62 (2002) | Bayer Research Center | 2D 3D TSV |
| 12039560 | 377 | Carbonic anhydrase inhibitors. Preparation of potent sulfonamides inhibitors incorporating bile acid tails. |
Bioorg Med Chem Lett 12: 1551-7 (2002) | Universit£ degli Studi di Firenze | 2D 3D TSV |
| 12036378 | 12 | One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization. |
J Med Chem 45: 2670-3 (2002) | Australian National University | 2D 3D TSV |
| 12036377 | 3 | Synthesis and antitumor activity of 1,5,6-substituted E-3-(2-chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones. |
J Med Chem 45: 2666-9 (2002) | Università di Bologna | 2D 3D TSV |
| 12036376 | 4 | Synthesis of (+)-cis-N-(4-isothiocyanatobenzyl)-N-normetazocine, an isothiocyanate derivative of N-benzylnormetazocine as acylant agent for the sigma(1) receptor. |
J Med Chem 45: 2662-5 (2002) | University of Catania | 2D 3D TSV |
| 12036375 | 25 | Structure-activity relationship studies of nordihydroguaiaretic acid inhibitors toward soybean, 12-human, and 15-human lipoxygenase. |
J Med Chem 45: 2659-61 (2002) | University of California | 2D 3D TSV |
| 12036374 | 2 | Sugar-modified conjugated diene analogues of adenosine and uridine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects. |
J Med Chem 45: 2651-8 (2002) | Florida International University | 2D 3D TSV |
| 12036373 | 72 | Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors. |
J Med Chem 45: 2644-50 (2002) | University of Arizona | 2D 3D TSV |
| 12036372 | 143 | Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits. |
J Med Chem 45: 2624-43 (2002) | Sphinx Laboratories | 2D 3D TSV |
| 12036368 | 59 | Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor. |
J Med Chem 45: 2589-98 (2002) | Yamanouchi Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12036367 | 46 | Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. |
J Med Chem 45: 2579-88 (2002) | University of Montpellier | 2D 3D TSV |
| 12036366 | 12 | Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
J Med Chem 45: 2571-8 (2002) | Universit£ degli Studi di Bologna | 2D 3D TSV |
| 12036362 | 6 | Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate. |
J Med Chem 45: 2534-42 (2002) | Arizona State University | 2D 3D TSV |
| 12036361 | 28 | Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones. |
J Med Chem 45: 2526-33 (2002) | Vrije Universiteit | 2D 3D TSV |
| 12036360 | 58 | Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones. |
J Med Chem 45: 2520-5 (2002) | Vrije Universiteit | 2D 3D TSV |
| 12036356 | 234 | Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups. |
J Med Chem 45: 2484-93 (2002) | Berlex Biosciences | 2D 3D TSV |
| 12036355 | 36 | Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water. |
J Med Chem 45: 2469-83 (2002) | University of Parma | 2D 3D TSV |
| 12036354 | 23 | Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. |
J Med Chem 45: 2454-68 (2002) | The Royal Danish School of Pharmacy | 2D 3D TSV |
| 12036353 | 38 | Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence. |
J Med Chem 45: 2432-53 (2002) | Pfizer Inc | 2D 3D TSV |
| 12036351 | 31 | Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. |
J Med Chem 45: 2417-24 (2002) | Pfizer Inc | 2D 3D TSV |
| 12036350 | 9 | Inhibition of MIF bioactivity by rational design of pharmacological inhibitors of MIF tautomerase activity. |
J Med Chem 45: 2410-6 (2002) | Institute for Medical Research | 2D 3D TSV |
| 12036349 | 58 | 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency. |
J Med Chem 45: 2388-409 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12036348 | 28 | SAR and X-ray. A new approach combining fragment-based screening and rational drug design: application to the discovery of nanomolar inhibitors of Src SH2. |
J Med Chem 45: 2379-87 (2002) | Aventis | 2D 3D TSV |
| 12036347 | 116 | Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes. |
J Med Chem 45: 2366-78 (2002) | Aventis Pharma Deutschland GmbH | 2D 3D TSV |
| 12036346 | 12 | 1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. |
J Med Chem 45: 2362-5 (2002) | TBA | 2D 3D TSV |
| 12036343 | 24 | Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors. |
J Med Chem 45: 2352-4 (2002) | TBA | 2D 3D TSV |
| 12031337 | 16 | CoMFA and HQSAR of acylhydrazide cruzain inhibitors. |
Bioorg Med Chem Lett 12: 1537-41 (2002) | Universidade Federal do Rio de Janeiro | 2D 3D TSV |
| 12031334 | 17 | Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. |
Bioorg Med Chem Lett 12: 1525-8 (2002) | Novo Nordisk A/S | 2D 3D TSV |
| 12031333 | 5 | Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B. |
Bioorg Med Chem Lett 12: 1521-3 (2002) | Georgetown University Medical Center | 2D 3D TSV |
| 12031332 | 27 | Nicotinanilides as inhibitors of neutrophil chemotaxis. |
Bioorg Med Chem Lett 12: 1517-20 (2002) | Celltech R&D Inc. | 2D 3D TSV |
| 12031331 | 48 | Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors. |
Bioorg Med Chem Lett 12: 1511-5 (2002) | Millennium Pharmaceuticals Inc | 2D 3D TSV |
| 12031329 | 110 | Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists. |
Bioorg Med Chem Lett 12: 1501-5 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12031328 | 21 | N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists. |
Bioorg Med Chem Lett 12: 1497-500 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12031323 | 16 | SAR and species/stereo-selective metabolism of the sorbitol dehydrogenase inhibitor, CP-470,711. |
Bioorg Med Chem Lett 12: 1477-80 (2002) | Pfizer Inc | 2D 3D TSV |
| 12031319 | 46 | Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. |
Bioorg Med Chem Lett 12: 1457-61 (2002) | Merck Frosst Centre for Therapeutic Research | 2D 3D TSV |
| 12031318 | 45 | CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
Bioorg Med Chem Lett 12: 1451-6 (2002) | Celltech R&D Ltd | 2D 3D TSV |
| 12031315 | 6 | Novel lipoic acid analogues that inhibit nitric oxide synthase. |
Bioorg Med Chem Lett 12: 1439-42 (2002) | Institute Henri Beaufour | 2D 3D TSV |
| 12023553 | 5 | Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs. |
J Pharmacol Exp Ther 301: 1179-89 (2002) | University of North Carolina at Chapel Hill | 2D 3D TSV |
| 12023552 | 11 | Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase. |
J Pharmacol Exp Ther 301: 1166-78 (2002) | University of North Carolina | 2D 3D TSV |
| 12023542 | 23 | Effects of norepinephrine and serotonin transporter inhibitors on hyperactivity induced by neonatal 6-hydroxydopamine lesioning in rats. |
J Pharmacol Exp Ther 301: 1097-102 (2002) | Harvard University | 2D 3D TSV |
| 12023506 | 4 | Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. |
J Pharmacol Exp Ther 301: 797-802 (2002) | Nagoya University School of Medicine | 2D 3D TSV |
| 12014973 | 3 | Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. |
J Med Chem 45: 2342-5 (2002) | Wyeth Research | 2D 3D TSV |
| 12014970 | 42 | Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging. |
J Med Chem 45: 2319-24 (2002) | Yale University | 2D 3D TSV |
| 12014967 | 25 | Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. |
J Med Chem 45: 2289-93 (2002) | Preclinical Research Novartis Pharma AG | 2D 3D TSV |
| 12014965 | 38 | Homodimeric tacrine congeners as acetylcholinesterase inhibitors. |
J Med Chem 45: 2277-82 (2002) | National Defense Medical Center | 2D 3D TSV |
| 12014964 | 19 | Synthesis and in vitro pharmacology of substituted quinoline-2,4-dicarboxylic acids as inhibitors of vesicular glutamate transport. |
J Med Chem 45: 2260-76 (2002) | The University of Montana | 2D 3D TSV |
| 12014961 | 287 | 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues. |
J Med Chem 45: 2229-39 (2002) | GlaxoSmithKline Research Laboratories | 2D 3D TSV |
| 12014960 | 10 | Mode of action of 4-hydroxyphenylpyruvate dioxygenase inhibition by triketone-type inhibitors. |
J Med Chem 45: 2222-8 (2002) | Tunghai University | 2D 3D TSV |
| 12014959 | 11 | Molecular docking and high-throughput screening for novel inhibitors of protein tyrosine phosphatase-1B. |
J Med Chem 45: 2213-21 (2002) | Pfizer Inc | 2D 3D TSV |
| 12014957 | 86 | 2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor. |
J Med Chem 45: 2197-206 (2002) | Meiji Seika Kaisha Ltd. | 2D 3D TSV |
| 12014956 | 34 | Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents. |
J Med Chem 45: 2185-96 (2002) | University of Illinois at Urbana-Champaign | 2D 3D TSV |
| 12014955 | 19 | An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors. |
J Med Chem 45: 2173-84 (2002) | Aventis Pharma S.A. | 2D 3D TSV |
| 12014954 | 32 | Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists. |
J Med Chem 45: 2160-72 (2002) | Novartis Institute for Medical Sciences | 2D 3D TSV |
| 12014953 | 3 | Rational design and evaluation of new lead compound structures for selective betaARK1 inhibitors. |
J Med Chem 45: 2150-9 (2002) | Daiichi Pharmaceutical Co., Ltd | 2D 3D TSV |
| 12014951 | 139 | Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. |
J Med Chem 45: 2131-8 (2002) | National Institute of Diabetes & Digestive & Kidney Diseases | 2D 3D TSV |
| 12014950 | 24 | Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity. |
J Med Chem 45: 2127-30 (2002) | TBA | 2D 3D TSV |
| 12014949 | 63 | Arylamidrazones as novel corticotropin releasing factor receptor antagonists. |
J Med Chem 45: 2123-6 (2002) | TBA | 2D 3D TSV |
| 12009900 | 67 | Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1. |
Biochemistry 41: 6383-90 (2002) | Merck Research Laboratories | 2D 3D TSV |
| 12005172 | 18 | Involvement of rat organic anion transporter 3 (rOAT3) in cephaloridine-induced nephrotoxicity: in comparison with rOAT1. |
Life Sci 70: 1861-74 (2002) | Kyorin University School of Medicine | 2D 3D TSV |
Curated by BindingDB
Curated by ChEMBL