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135 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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.EBI 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 LockeEBI 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).EBI Janssen Research& Development
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.EBI Janssen Pharmaceutical Research& Development, LLC
27660692 70 Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-┐ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.EBI Infinity Pharmaceuticals, Inc.
27326332 66 Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.EBI Bristol-Myers Squibb Company
26914985 124 Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.EBI Boehringer Ingelheim RCV GmbH& Co KG
27190604 26 Discovery of Potent, Orally Bioavailable Inhibitors of Human Cytomegalovirus.EBI Boehringer Ingelheim (Canada) Ltd.
26985323 5 Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.EBI Merck Research Laboratories
26985314 23 Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain A▀ Reduction in Rodents.EBI Bristol-Myers Squibb Company
26924461 45 Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.EBI 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.EBI Lilly Research Laboratories
27055941 19 Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).EBI Bristol-Myers Squibb Research and Development
26709102 142 Discovery of Vibegron: A Potent and Selective▀3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.EBI 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.EBI Lilly Research Laboratories
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.EBI Pfizer Inc.
26363868 10 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents.EBI NorthShore University HealthSystem
25978966 65 Development of a novel class of potent and selective FIXa inhibitors.EBI 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.EBI AstraZeneca
26288692 37 Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.EBI Bristol Myers-Squibb Research and Development
26191360 99 Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.EBI 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).EBI Heptares Therapeutics Ltd.
26191364 10 Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.EBI 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.EBI Boehringer Ingelheim Pharma GmbH& Co. KG
26091726 41 Discovery and characterization of a potent and selective EP4 receptor antagonist.EBI Lilly Research Laboratories
22328583 132 Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.EBI Pfizer Inc.
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.EBI Eisai Co., Ltd.
26087021 94 Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.EBI TBA
26005524 147 Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.EBI 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.EBI Seragon Pharmaceuticals
21289076 2 Reevaluation of the microsomal metabolism of montelukast: major contribution by CYP2C8 at clinically relevant concentrations.EBI University of Helsinki
23118326 5 Clinical pharmacokinetics, metabolism, and drug-drug interaction of carfilzomib.EBI 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.EBI 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.EBI Pfizer Inc.
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.EBI Amgen, Inc
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.EBI 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.EBI The Scripps Research Institute
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
25050169 52 Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11▀-Hydroxysteroid Dehydrogenase Type 1 (11▀-HSD-1).EBI Bristol-Myers Squibb
24980053 153 Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.EBI Bristol-Myers Squibb Company
25556092 85 Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.EBI Boehringer Ingelheim Pharma GmbH& Co. KG
25453808 101 Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.EBI Bristol-Myers Squibb Company
25330343 49 Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.EBI Translational Research Institute
25310383 50 Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.EBI 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.EBI Chinese Academy of Sciences
24900876 56 Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.EBI AstraZeneca
24685542 67 Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI Bristol-Myers Squibb Research and Development
24428186 10 Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione┐-secretase modulators.EBI Pfizer Inc.
24530032 65 Structure-based optimization of cyclopropyl urea derivatives as potent soluble epoxide hydrolase inhibitors for potential decrease of renal injury without hypotensive action.EBI Dainippon Sumitomo Pharma Co., Ltd
24252545 12 Discovery of an irreversible HCV NS5B polymerase inhibitor.EBI Merck Research Laboratories
24090135 201 Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication.EBI Sanofi
23973211 145 Fragment-based discovery of focal adhesion kinase inhibitors.EBI Merck KGaA
23896611 16 Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents.EBI 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.EBI Merck Research Laboratories
23664879 73 Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.EBI 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.EBI AstraZeneca
16248836 154 Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.EBI F. Hoffmann-La Roche Ltd.
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.EBI Pfizer Inc.
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.EBI ArQule Inc.
22409598 28 Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.EBI Pfizer Inc.
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 ofEBI Pfizer Inc.
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).EBI 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.EBI Merck Research Laboratories
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
22938786 86 Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.EBI Dainippon Sumitomo Pharma Co., Ltd
22185670 73 Oxadiazoles in medicinal chemistry.EBI AstraZeneca
22542012 155 The design, synthesis, and biological evaluation of PIM kinase inhibitors.EBI Exelixis
22239545 287 Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19.EBI Amgen Inc.
22361135 29 Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists.EBI 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]pyrEBI Pfizer Inc.
21316976 62 17,20-lyase inhibitors. Part 4: design, synthesis and structure-activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors.EBI Takeda Pharmaceutical Company, Ltd
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.EBI University of Liverpool
18462007 7 Selective inhibition of aromatase by a dihydroisocoumarin from Xyris pterygoblephara.EBI 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.EBI Novartis Institutes for BioMedical Research
17201408 91 Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.EBI Wyeth Research
22070604 150 Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators.EBI 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.EBI Takeda Pharmaceutical Company, Ltd.
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.EBI Dainippon Sumitomo Pharma Co. Ltd
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.EBI Merck Research Laboratories
21147532 82 Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.EBI Merck Research Laboratories
19029327 7 In vitro and in vivo studies to characterize the clearance mechanism and potential cytochrome P450 interactions of anidulafungin.EBI Pfizer Inc.
21036042 7 Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.EBI Pfizer Inc.
20942471 79 First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.EBI Genkyotex, S.A.
20797855 63 PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.EBI Pfizer Inc.
20452209 64 Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.EBI 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.EBI 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.EBI 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).EBI 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.EBI Merck Research Laboratories
19682899 211 Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.EBI Merck Research Laboratories
19541481 57 Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI Bristol-Myers Squibb Company
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.EBI 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.EBI 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.EBI Pfizer Global Research and Development
19222165 36 Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.EBI University of Liverpool
19447613 9 Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.EBI Merck Research Laboratories
19354254 24 Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.EBI Merck Research Laboratories
19320488 171 1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.EBI Merck Research Laboratories
19309152 81 Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.EBI Merck Research Laboratories
18477506 7 Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.EBI Merck Research Laboratories
17705360 76 Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.EBI Wyeth Research
17399990 45 In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).EBI Université Laval
16495056 23 Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.EBI Universite Paris 5 René Descartes
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.EBI Université Paris V