The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28686445 |
39 |
Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension. |
Sun Yat-Sen University |
| 28359790 |
110 |
Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors. |
Takeda California |
| 28274629 |
76 |
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism. |
Hanyang University |
| 28230986 |
7 |
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease. |
Forum Pharmaceuticals |
| 28212021 |
111 |
Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT |
Suven Life Sciences |
| 28038328 |
17 |
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
East China University Of Science And Technology |
| 28072531 |
120 |
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
Arena Pharmaceuticals |
| 28337332 |
41 |
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. |
Bristol-Myers Squibb |
| 28337324 |
14 |
Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. |
Global Blood Therapeutics |
| 28003141 |
65 |
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors. |
Bristol-Myers Squibb Research And Development |
| 28169164 |
19 |
Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors. |
Takeda California |
| 27958732 |
93 |
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship. |
Bristol-Myers Squibb |
| 27583770 |
82 |
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke |
Bristol-Myers Squibb Research And Development |
| 27579727 |
33 |
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
Janssen Pharmaceutica |
| 27548392 |
76 |
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor. |
Janssen Research And Development |
| 27660692 |
70 |
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. |
Infinity Pharmaceuticals |
| 27326332 |
66 |
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist. |
Bristol-Myers Squibb |
| 26914985 |
124 |
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. |
Boehringer Ingelheim Rcv |
| 27190604 |
26 |
Discovery of Potent, Orally Bioavailable Inhibitors of Human Cytomegalovirus. |
Boehringer Ingelheim (Canada) |
| 26985323 |
5 |
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors. |
Merck Research Laboratories |
| 26985314 |
23 |
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents. |
Bristol-Myers Squibb |
| 26924461 |
45 |
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series. |
Bristol-Myers Squibb Research And Development |
| 27020304 |
31 |
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists. |
Eli Lilly |
| 27055941 |
19 |
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1). |
Bristol-Myers Squibb Research And Development |
| 26709102 |
142 |
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder. |
Merck Research Laboratories |
| 26764191 |
38 |
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile. |
Eli Lilly |
| 26509551 |
31 |
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases. |
Pfizer |
| 26363868 |
10 |
3-Nitrotriazole-based piperazides as potent antitrypanosomal agents. |
Northshore University Healthsystem |
| 25978966 |
65 |
Development of a novel class of potent and selective FIXa inhibitors. |
Merck Research Laboratories |
| 26313252 |
22 |
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
Astrazeneca |
| 26288692 |
37 |
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer. |
Bristol-Myers Squibb Research And Development |
| 26191360 |
99 |
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation. |
Merck Research Laboratories |
| 26225459 |
48 |
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile). |
Heptares Therapeutics |
| 26191364 |
10 |
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer. |
Bristol-Myers Squibb Research |
| 26105194 |
24 |
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908. |
Boehringer Ingelheim Pharma |
| 26091726 |
41 |
Discovery and characterization of a potent and selective EP4 receptor antagonist. |
Eli Lilly |
| 22328583 |
132 |
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
Pfizer |
| 25953512 |
74 |
Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist. |
Eisai |
| 26087021 |
94 |
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate. |
TBA |
| 26005524 |
147 |
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. |
Merck Research Laboratories |
| 25879485 |
60 |
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
Seragon Pharmaceuticals |
| 21289076 |
2 |
Reevaluation of the microsomal metabolism of montelukast: major contribution by CYP2C8 at clinically relevant concentrations. |
University Of Helsinki |
| 23118326 |
5 |
Clinical pharmacokinetics, metabolism, and drug-drug interaction of carfilzomib. |
Onyx Pharmaceuticals |
| 22496391 |
40 |
Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human. |
Bristol-Myers Squibb Research |
| 22645092 |
15 |
Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs. |
Pfizer |
| 22930276 |
25 |
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. |
Amgen |
| 23132334 |
28 |
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor. |
Glaxosmithkline |
| 25781223 |
96 |
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors. |
The Scripps Research Institute |
| 25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
Eberhard Karls Universit£T T£Bingen |
| 25050169 |
52 |
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1). |
Bristol-Myers Squibb |
| 24980053 |
153 |
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. |
Bristol-Myers Squibb |
| 25556092 |
85 |
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds. |
Boehringer Ingelheim Pharma |
| 25453808 |
101 |
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. |
Bristol-Myers Squibb |
| 25330343 |
49 |
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
Translational Research Institute |
| 25310383 |
50 |
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition. |
Novartis Institutes For Biomedical Research |
| 25179681 |
81 |
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor. |
Chinese Academy Of Sciences |
| 24900876 |
56 |
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
Astrazeneca |
| 24900838 |
30 |
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor. |
Merck Research Laboratories |
| 24685542 |
67 |
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases. |
Bristol-Myers Squibb Research And Development |
| 24428186 |
10 |
Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione¿-secretase modulators. |
Pfizer |
| 24530032 |
65 |
Structure-based optimization of cyclopropyl urea derivatives as potent soluble epoxide hydrolase inhibitors for potential decrease of renal injury without hypotensive action. |
Dainippon Sumitomo Pharma |
| 24900630 |
16 |
Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
University Of Cape Town |
| 24252545 |
12 |
Discovery of an irreversible HCV NS5B polymerase inhibitor. |
Merck Research Laboratories |
| 24900593 |
45 |
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. |
Glaxosmithkline |
| 24090135 |
201 |
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication. |
Sanofi |
| 23973211 |
145 |
Fragment-based discovery of focal adhesion kinase inhibitors. |
Merck |
| 23896611 |
16 |
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. |
University Of Cape Town |
| 23808489 |
11 |
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways. |
Merck Research Laboratories |
| 23664879 |
73 |
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase. |
Glaxosmithkline |
| 23200256 |
54 |
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor. |
Astrazeneca |
| 16248836 |
154 |
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
F. Hoffmann-La Roche |
| 22651823 |
57 |
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
Pfizer |
| 22533986 |
181 |
Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. |
Arqule |
| 22409598 |
28 |
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
Pfizer |
| 22924734 |
87 |
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of |
Pfizer |
| 22784008 |
100 |
Synthesis and biological evaluation of the 1-arylpyrazole class ofs(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). |
Esteve |
| 22708876 |
106 |
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes. |
Merck Research Laboratories |
| 22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
| 22938786 |
86 |
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
Dainippon Sumitomo Pharma |
| 22185670 |
73 |
Oxadiazoles in medicinal chemistry. |
Astrazeneca |
| 24900436 |
18 |
Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. |
TBA |
| 22328963 |
4 |
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity. |
TBA |
| 24900359 |
31 |
Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists. |
TBA |
| 22542012 |
155 |
The design, synthesis, and biological evaluation of PIM kinase inhibitors. |
Exelixis |
| 24900284 |
129 |
Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids. |
TBA |
| 22239545 |
287 |
Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19. |
Amgen |
| 22361135 |
29 |
Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists. |
Lundbeck Research Usa |
| 21438541 |
45 |
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyr |
Pfizer |
| 21316976 |
62 |
17,20-lyase inhibitors. Part 4: design, synthesis and structure-activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors. |
Takeda Pharmaceutical |
| 19284751 |
26 |
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable"back-up" compound for N-tert-butyl isoquine. |
University Of Liverpool |
| 18462007 |
7 |
Selective inhibition of aromatase by a dihydroisocoumarin from Xyris pterygoblephara. |
Universidade Federal De Minas Gerais |
| 17630726 |
32 |
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration. |
Novartis Institutes For Biomedical Research |
| 17201408 |
91 |
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists. |
Wyeth Research |
| 22070604 |
150 |
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators. |
Merck Research Laboratories |
| 21978946 |
45 |
Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer. |
Takeda Pharmaceutical |
| 21865048 |
29 |
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. |
Dainippon Sumitomo Pharma |
| 21411321 |
28 |
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate. |
Merck Research Laboratories |
| 21147532 |
82 |
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core. |
Merck Research Laboratories |
| 19029327 |
7 |
In vitro and in vivo studies to characterize the clearance mechanism and potential cytochrome P450 interactions of anidulafungin. |
Pfizer |
| 21036042 |
7 |
Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK. |
Pfizer |
| 20942471 |
79 |
First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. |
Genkyotex |
| 20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
| 20452209 |
64 |
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A. |
Merck Research Laboratories |
| 20423086 |
93 |
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity. |
Merck Research Laboratories |
| 20223663 |
100 |
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. |
Wyeth Research |
| 20218621 |
131 |
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453). |
Bristol-Myers Squibb |
| 20184326 |
40 |
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate. |
Merck Research Laboratories |
| 19682899 |
211 |
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors. |
Merck Research Laboratories |
| 19541481 |
57 |
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb |
| 19719241 |
55 |
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. |
Wyeth Research |
| 19537798 |
22 |
Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate. |
Tsukuba Research Institute |
| 19209845 |
12 |
Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor. |
Pfizer |
| 19222165 |
36 |
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
University Of Liverpool |
| 19447613 |
9 |
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides. |
Merck Research Laboratories |
| 19354254 |
24 |
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. |
Merck Research Laboratories |
| 19320488 |
171 |
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity. |
Merck Research Laboratories |
| 19309152 |
81 |
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats. |
Merck Research Laboratories |
| 18477506 |
7 |
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists. |
Merck Research Laboratories |
| 17705360 |
76 |
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site. |
Wyeth Research |
| 17399990 |
45 |
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2). |
Université |
| 16495056 |
23 |
Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2. |
Universite Paris 5 René |
| 11606127 |
96 |
Synthesis of sulfaphenazole derivatives and their use as inhibitors and tools for comparing the active sites of human liver cytochromes P450 of the 2C subfamily. |
Université |
| 28209465 |
124 |
Identification of highly potent and selective PI3K? inhibitors. |
Bristol-Myers Squibb |
| 28653847 |
9 |
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8). |
Celgene |
| 28557445 |
11 |
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. |
Bayer |
| 28541707 |
119 |
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders. |
Bristol-Myers Squibb |
| 28537398 |
114 |
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11?-Hydroxysteroid Dehydrogenase Type 1 Inhibitor. |
Bristol-Myers Squibb |
| 28430437 |
19 |
Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies. |
Bristol-Myers Squibb Research And Development |
| 28418664 |
32 |
Selective I |
Bristol-Myers Squibb |
| 19041240 |
41 |
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. |
Wyeth Research |
| 16451071 |
44 |
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1). |
Duquesne University |
| 16620080 |
15 |
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors. |
Purdue University |
| 7683725 |
30 |
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
Merck Research Laboratories |
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Cycloalkylpiperazines as HIV-1 Protease Inhibitors: Enhanced Oral Absorption |
Merck Research Laboratories |
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