523 articles for thisTarget
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Article Title
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Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT
Bristol-Myers Squibb
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Bristol-Myers Squibb
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors.
Bristol-Myers Squibb
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.
Bristol-Myers Squibb
CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine.
Bristol-Myers Squibb
Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.
Bristol-Myers Squibb
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
Bristol-Myers Squibb
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
Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.
Bristol-Myers Squibb
Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Bristol-Myers Squibb
Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.
Bristol-Myers Squibb
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.
Bristol-Myers Squibb
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
Bristol-Myers Squibb
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents.
Bristol-Myers Squibb
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Bristol-Myers Squibb
Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based¿-secretase modulators.
Bristol-Myers Squibb
Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Bristol-Myers Squibb
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.
Bristol-Myers Squibb
Macrocyclic prolinyl acyl guanidines as inhibitors ofß-secretase (BACE).
Bristol-Myers Squibb
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.
Bristol-Myers Squibb
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Bristol-Myers Squibb
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Bristol-Myers Squibb
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
Bristol-Myers Squibb
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Bristol-Myers Squibb
Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology.
Bristol-Myers Squibb
Metabolism and disposition of [14C]brivanib alaninate after oral administration to rats, monkeys, and humans.
Bristol-Myers Squibb
Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of thed-opioid receptor.
Bristol-Myers Squibb
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Bristol-Myers Squibb
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Bristol-Myers Squibb
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.
Bristol-Myers Squibb
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Bristol-Myers Squibb
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
Bristol-Myers Squibb
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
Bristol-Myers Squibb
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRß.
Bristol-Myers Squibb
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Bristol-Myers Squibb
Discovery of pyridyl sulfonamide 11-beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors for the treatment of metabolic disorders.
Bristol-Myers Squibb
Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.
Bristol-Myers Squibb
Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.
Bristol-Myers Squibb
2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.
Bristol-Myers Squibb
Synthesis and structure-activity relationship of dihydrobenzofuran derivatives as novel human GPR119 agonists.
Bristol-Myers Squibb
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.
Bristol-Myers Squibb
Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.
Bristol-Myers Squibb
Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.
Bristol-Myers Squibb
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors.
Bristol-Myers Squibb
Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1).
Bristol-Myers Squibb
Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.
Bristol-Myers Squibb
Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.
Bristol-Myers Squibb
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.
Bristol-Myers Squibb
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Bristol-Myers Squibb
Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.
Bristol-Myers Squibb
Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.
Bristol-Myers Squibb
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.
Bristol-Myers Squibb
2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.
Bristol-Myers Squibb
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Bristol-Myers Squibb
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Bristol-Myers Squibb
Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.
Bristol-Myers Squibb
Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.
Bristol-Myers Squibb
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Bristol-Myers Squibb
Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
Bristol-Myers Squibb
Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors.
Bristol-Myers Squibb
Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.
Bristol-Myers Squibb
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Bristol-Myers Squibb
Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Bristol-Myers Squibb
Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.
Bristol-Myers Squibb
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.
Bristol-Myers Squibb
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Bristol-Myers Squibb
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.
Bristol-Myers Squibb
Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.
Bristol-Myers Squibb
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Bristol-Myers Squibb
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Bristol-Myers Squibb
Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
Bristol-Myers Squibb
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
Bristol-Myers Squibb
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Bristol-Myers Squibb
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Bristol-Myers Squibb
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.
Bristol-Myers Squibb
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Bristol-Myers Squibb
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
Bristol-Myers Squibb
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
Bristol-Myers Squibb
Triketoacid inhibitors of HIV-integrase: a new chemotype useful for probing the integrase pharmacophore.
Bristol-Myers Squibb
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.
Bristol-Myers Squibb
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
Bristol-Myers Squibb
Synthesis, biological profile, and quantitative structure-activity relationship of a series of novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors.
Bristol-Myers Squibb
Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1).
Bristol-Myers Squibb
Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2).
Bristol-Myers Squibb
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Monosubstituted¿-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors ofß-secretase (BACE).
Bristol-Myers Squibb
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.
Bristol-Myers Squibb
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791
Bristol-Myers Squibb
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.
Bristol-Myers Squibb
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1).
Bristol-Myers Squibb
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
Bristol-Myers Squibb
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Bristol-Myers Squibb
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Bristol-Myers Squibb
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.
Bristol-Myers Squibb
Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Bristol-Myers Squibb
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.
Bristol-Myers Squibb
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
Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Bristol-Myers Squibb
Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles.
Bristol-Myers Squibb
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Bristol-Myers Squibb
Dihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists.
Bristol-Myers Squibb
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Bristol-Myers Squibb
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Bristol-Myers Squibb
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Bristol-Myers Squibb
Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.
Bristol-Myers Squibb
Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.
Bristol-Myers Squibb
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Bristol-Myers Squibb
Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.
Bristol-Myers Squibb
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Bristol-Myers Squibb
Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR).
Bristol-Myers Squibb
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.
Bristol-Myers Squibb
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Bristol-Myers Squibb
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Bristol-Myers Squibb
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Bristol-Myers Squibb
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
Bristol-Myers Squibb
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).
Bristol-Myers Squibb
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bristol-Myers Squibb
Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.
Bristol-Myers Squibb
The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Bristol-Myers Squibb
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Bristol-Myers Squibb
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Bristol-Myers Squibb
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Bristol-Myers Squibb
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead.
Bristol-Myers Squibb
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO).
Bristol-Myers Squibb
Identification of 6-hydroxy-5-phenyl sulfonylpyrimidin-4(1H)-one APJ receptor agonists.
Bristol-Myers Squibb
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.
Bristol-Myers Squibb
Design and synthesis of potent, non-peptide inhibitors of HCV NS3 protease.
Bristol-Myers Squibb
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.
Bristol-Myers Squibb
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors.
Bristol-Myers Squibb
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P
Bristol-Myers Squibb
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Bristol-Myers Squibb
Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase.
Bristol-Myers Squibb
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.
Bristol-Myers Squibb
CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.
Bristol-Myers Squibb
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Bristol-Myers Squibb
Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Bristol-Myers Squibb
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.
Bristol-Myers Squibb
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.
Bristol-Myers Squibb
Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.
Bristol-Myers Squibb
Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine β-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.
Bristol-Myers Squibb
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.
Bristol-Myers Squibb
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Bristol-Myers Squibb
Benzothiazole-based compounds as potent endothelial lipase inhibitors.
Bristol-Myers Squibb
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.
Bristol-Myers Squibb
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.
Bristol-Myers Squibb
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
Bristol-Myers Squibb
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.
Bristol-Myers Squibb
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Bristol-Myers Squibb
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Bristol-Myers Squibb
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
Bristol-Myers Squibb
Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.
Bristol-Myers Squibb
Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.
Bristol-Myers Squibb
Discovery of novel P1 groups for coagulation factor VIIa inhibition using fragment-based screening.
Bristol-Myers Squibb
Synthesis and SAR studies of novel heteroaryl fused tetracyclic indole-diamide compounds: potent allosteric inhibitors of the hepatitis C virus NS5B polymerase.
Bristol-Myers Squibb
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bristol-Myers Squibb
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Bristol-Myers Squibb
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.
Bristol-Myers Squibb
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor.
Bristol-Myers Squibb
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).
Bristol-Myers Squibb
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
The discovery and optimization of naphthalene-linked P2-P4 Macrocycles as inhibitors of HCV NS3 protease.
Bristol-Myers Squibb
Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor.
Bristol-Myers Squibb
Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.
Bristol-Myers Squibb
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Bristol-Myers Squibb
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.
Bristol-Myers Squibb
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Bristol-Myers Squibb
Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Bristol-Myers Squibb
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Bristol-Myers Squibb
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 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.
Bristol-Myers Squibb
COMPOSITION FOR PREVENTING OR TREATING GRAVES' DISEASE COMPRISING COMPOUND CONTAINING AN IMIDAZOPYRIDINE STRUCTURE AS ACTIVE INGREDIENT
Esgelbio
Modulators of programmed death-ligand-1 and/or programmed death-ligand-2
Southern Research Institute
NAMPT ACTIVATORS FOR TREATING METABOLIC AND NEUROLOGICAL DISORDERS
University of Illinois
SUBSTITUTED 1-ARYL-1’-HETEROARYL COMPOUNDS, SUBSTITUTED 1,1’-BIHETEROARYL COMPOUNDS, AND METHODS USING SAME
Arbutus Biopharma
Quinazoline Derivatives, Pharmaceutical Compositions, and Therapeutic Uses Related to Nox Inhibition
Emory University
Preparation for 6-amino-1H-pyrazolo[3,4-d]pyrimidine-based JAK kinase inhibitor and application thereof
Peking Union Medical College
N-(BENZOYL)-PHENYLALANINE COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF
Hangzhou Apeloa Medicine Research Institute Co.
Inhibitors of bacterial glutaminyl cyclases for use in the treatment of periodontal and related diseases
Fraunhofer-Gesellschaft Zur Forderung Der Angewandten Forschung
Inhibitors of glycogen synthase 1 (GYS1) and methods of use thereof
Maze Therapeutics
N-((1-BENZYLPIPERIDIN-3-YL)METHYL)-N-(2-METHOXYETHYL)NAPHTHALENE-2-SULFONAMIDE FOR THE TREATMENT OF CANINE COGNITIVE DYSFUNCTION AND OTHER FORMS OF DEMENTIA IN DOGS
Univerza V Ljubljani
Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
Revolution Medicines
Method for preparing pyrrolidinyl urea derivative
Zhangzhou Pien Tze Huang Pharmaceutical
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer
The Institute of Cancer Research: Royal Cancer Hospital
RIP1 inhibitory compounds and methods for making and using the same
Rigel Pharmaceuticals
Protacs based on VHL ligand targeting coronavirus 3CL protease and preparation method and application thereof
Shaanxi Panlong Pharmaceutical
Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
Array Biopharma
Pyrimidine JAK inhibitors for the treatment of skin diseases
Theravance Biopharma R&D Ip
Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof
La Jolla Institute of Allergy & Immunology
2-quinolone derived inhibitors of BCL6
The Institute of Cancer Research: Royal Cancer Hospital
Cyanopyrrolidine derivatives with activity as inhibitors of USP30
Mission Therapeutics
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
Substituted pyrrolidines as G-protein coupled receptor 43 agonists
Epics Therapeutics
2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors
Ideaya Biosciences
Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR
Blueprint Medicines
JAK kinase inhibitor compounds for treatment of respiratory disease
Theravance Biopharma R&D Ip
Phosphonate linkers and their use to facilitate cellular retention of compounds
Merck Sharp & Dohme
3-((hetero-)aryl)-alkyl-8-amino-2-oxo-l,3-diaza-spiro-[4.5]-decane derivatives
Gruenenthal
Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders
Achillion Pharmaceuticals
Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
Merck Sharp & Dohme
Diaminopyrimidine benzenesulfone derivatives and uses thereof
Dana-Farber Cancer Institute
Compounds as neuronal histamine receptor-3 antagonists and uses thereof
Xw Laboratories
Selective Bruton's tyrosine kinase inhibitor and use thereof
Hangzhou Hertz Pharmaceutical
Benzenesulfonamide compounds and their use as therapeutic agents
Xenon Pharmaceuticals
Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors
Merck Sharp & Dohme
Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
Jenrin Discovery
HYPDH inhibitors and methods of use for the treatment of kidney stones
Wake Forest University Health Sciences
Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (SSTR4) agonists
Boehringer Ingelheim International
4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators
Vanderbilt University
6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1H)-one as APJ agonists
Bristol-Myers Squibb
Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
Forma Therapeutics
Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
Enanta Pharmaceuticals
2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs
Bayer Pharma Aktiegesellschaft
(Hetero)aryl imidazoles/pyrazoles for treatment of neurological disorders
Hoffmann-La Roche
4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
Boehringer Ingelheim International
Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators
Beigene
Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use
Merck Sharp & Dohme
PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
Mitobridge
Substituted oxopyridine derivatives and use thereof cardiovascular disorders
Bayer Pharma Aktiengesellschaft
Heterocyclic compounds, process for preparation of the same and use thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
Sulfone amide linked benzothiazole inhibitors of endothelial lipase
Bristol-Myers Squibb
Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization
Newlink Genetics
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma
1,2,3-triazole-4-amine derivatives for the treatment of sigma receptor related diseases and disorders
Laboratorios Del Dr. Esteve
Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
University of North Carolina At Chapel Hill
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
Shionogi
2-oxothiazole compounds and method of using same for chronic inflammatory disorders
Avexxin
Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
Effector Therapeutics
Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer
Kainos Medicine
Sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of virus infection
Hoffmann-La Roche
2-pyridinecarboxamide derivatives, compositions containing such compounds, and methods of treatment
Merck Sharp & Dohme
Augmenting moieties for anti-inflammatory compounds
Rutgers, The State University of New Jersey
In vitro effects of cinnamic acid derivatives on protein tyrosine phosphatase 1B.
Chulalongkorn University
Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor.
Federal University of Sao Paulo
Tripeptides with non-code amino acids as potential serine proteases inhibitors.
Medical University of Bialystok
Secondary/tertiary benzenesulfonamides with inhibitory action against the cytosolic human carbonic anhydrase isoforms I and II.
Ataturk University
Effects of some drugs on human cord blood erythrocyte carbonic anhydrases I and II: an in vitro study.
Erzincan University
In vitro effects of some drugs on human erythrocyte glutathione reductase.
Ataturk University
3-arylidene-5-(4-isobutylphenyl)-2(3H)-furanones: a new series of anti-inflammatory and analgesic compounds having antimicrobial activity.
Jamia Hamdard
Stereoselective inhibition of butyrylcholinesterase by enantiomers of exo- and endo-2-norbornyl-N-n-butylcarbamates.
Chung Shan Medical University Hospital
Structure-based rational design of self-inhibitory peptides to disrupt the intermolecular interaction between the troponin subunits C and I in neuropathic pain.
The Affiliated Hospital of Qingdao University
Exploiting sp(2) -Hybridisation in the Development of Potent 1,5-a-l-Arabinanase Inhibitors.
University of Western Australia
Oxysterol-binding protein (OSBP)-related protein 4 (ORP4) is essential for cell proliferation and survival.
Dalhousie University
Structural basis of pharmacological chaperoning for human ß-galactosidase.
The University of Tokyo
Method for dual inhibition of SGLT1 and SGLT2 using diphenylmethane derivatives
Green Cross
Selective β-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents
University of North Carolina At Chapel Hill
Coregulator control of androgen receptor action by a novel nuclear receptor-binding motif.
Karlsruhe Institute of Technology
Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.
University of Texas Southwestern Medical Center
Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitors
Taibah University
Interaction of Azole-Based Environmental Pollutants with the Coelomic Hemoglobin from Amphitrite ornata: A Molecular Basis for Toxicity.
North Carolina State University
Small Molecules Engage Hot Spots through Cooperative Binding To Inhibit a Tight Protein-Protein Interaction.
Indiana University School of Medicine
Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer's disease.
Sichuan University
Thymidine esters as substrate analogue inhibitors of angiogenic enzyme thymidine phosphorylase in vitro.
University of Karachi
Symmetrical aryl linked bis-iminothiazolidinones as new chemical entities for the inhibition of monoamine oxidases: Synthesis, in vitro biological evaluation and molecular modelling analysis.
Quaid-I-Azam University
Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches.
Sanofi Oncology
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.
Glaxosmithkline
Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
Acetylon Pharmaceuticals
Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
Dana-Farber Cancer Institute
Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof
President and Fellows of Harvard College
A Unique Mdm2-Binding Mode of the 3-Pyrrolin-2-one- and 2-Furanone-Based Antagonists of the p53-Mdm2 Interaction.
Jagiellonian University
Rapid synthesis of flavone-based monoamine oxidase (MAO) inhibitors targeting two active sites using click chemistry.
Zhejiang University of Technology
Designed Small-Molecule Inhibitors of the Anthranilyl-CoA Synthetase PqsA Block Quinolone Biosynthesis in Pseudomonas aeruginosa.
East Carolina University
Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
Bristol-Myers Squibb
IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors
Institut De Ge��Ne��Tique Et De Biologie Mole��Culaire Et Cellulaire
Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.
University of Waterloo
Design, synthesis, cytotoxicity, HuTopoIIa inhibitory activity and molecular docking studies of pyrazole derivatives as potential anticancer agents.
Jamia Millia Islamia (A Central University)
Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.
Tehran University of Medical Sciences
Method for the treatment of pompe disease using 1-deoxynojirimycin and derivatives
Amicus Therapeutics
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.
University of Washington
Functionally selective ligands of dopamine D2 receptors
University of North Carolina At Chapel Hill
5,8-dihydro-6H-pyrazolo[3,4-h]quinazolines as IGF-1R/IR inhibitors
Boehringer Ingelheim International
Sulfoximine substituted quinazolines for pharmaceutical compositions
Boehringer Ingelheim International
Use of inhibitors of porphobilinogen deaminase in the treatment of congenital erythropoietic porphyria
AsociacióN Centro De InvestigacióN Cooperativa En Biociencias—Cic Biogune
Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as a-glucosidase inhibitors.
Jishou University
Substituted benzimidazole and imidazopyridine compounds useful as CYP17 modulators
Bristol-Meyers Squibb
Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity.
Panjab University
Evaluation of 2-indolcarbohydrazones as potent a-glucosidase inhibitors, in silico studies and DFT based stereochemical predictions.
Universiti Teknologi Mara (Uitm)
Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
Boehringer Ingelheim International
Indazolyl-substituted dihydroisoxa-zolopyridines and methods of use thereof
Bayer Intellectual Property
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
Birla Institute of Technology
Activity based probes (ABPs) interacting with glycosidases
Academisch Medisch Centrum Bij Universiteit Van Amsterdam
Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use
Merck Sharp & Dohme
Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors.
Technische Universit������T Dortmund
Synthesis and evaluation of a new series of 3,5-bis((5-bromo-6-methyl-2-t-aminopyrimidin-4-yl)thio)-4H-1,2,4-triazol-4-amines and their cyclized products 'pyrimidinylthio pyrimidotriazolothiadiazines' as 15- lipo-oxygenase inhibitors.
Ferdowsi University of Mashhad
Synthesis, biological evaluation, and docking studies of novel thiourea derivatives of bisindolylmethane as carbonic anhydrase II inhibitor.
Universiti Teknologi Mara (Uitm)
Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease
Merck Sharp & Dohme
Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions
Boehringer Ingelheim International
Substituted pyrimidines for the treatment of diseases such as cancer
Boehringer Ingelheim International
3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents
Boehringer Ingelheim International
Structure and function of PA4872 from Pseudomonas aeruginosa, a novel class of oxaloacetate decarboxylase from the PEP mutase/isocitrate lyase superfamily.
University of Maryland Biotechnology Institute
Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.
Moffitt Cancer Center
Type II Ligands as Chemical Auxiliaries To Favor Enzymatic Transformations by P450 2E1.
Mcgill University
Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding.
Academia Sinica
Novel Cruzain Inhibitors for the Treatment of Chagas' Disease.
University of California San Diego
N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors.
University of Kansas
Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.
Memorial Sloan-Kettering Cancer Center
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.
Purdue Pharma Discovery Research
FE200041 (D-Phe-D-Phe-D-Nle-D-Arg-NH2): A peripheral efficacious kappa opioid agonist with unprecedented selectivity.
University of Arizona
Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats.
Eli Lilly
Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.
Cornell University
Activity of opioid ligands in cells expressing cloned mu opioid receptors.
Molecular Research Institute
Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications.
Nih
Carbonic anhydrase activity modulators: synthesis of inhibitors and activators incorporating 2-substituted-thiazol-4-yl-methyl scaffolds.
UniversitÀ
Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.
St. Bartholomew'S and The Royal London School of Medicine and Dentistry
[3H]-Mesulergine labels 5-HT7 sites in rat brain and guinea-pig ileum but not rat jejunum.
Monash University
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Smithkline Beecham Pharmaceuticals
A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides.
University of Toronto
Cloning and pharmacologic characterization of a thromboxane A2 receptor from K562 (human chronic myelogenous leukemia) cells.
University of Cincinnati
Biochemical and pharmacological characterization of high-affinity trimetoquinol analogs on guinea pig and human beta adrenergic receptor subtypes: evidence for partial agonism.
Ohio State University
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.
University of Queensland Brisbane
RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.
Syntex Discovery Research
Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.
Vernalis (R&D)
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.
National Institute of Mental Health
2',3'-Dideoxy-N6-cyclohexyladenosine: an adenosine derivative with antagonist properties at adenosine receptors.
Pharmakologisches Institut
1-(m-chlorophenyl)piperazine (mCPP) interactions with neurotransmitter receptors in the human brain.
Stanford University
Characterization of the binding of [3H]muscimol, a potent gamma-aminobutyric acid agonist, to rat brain synaptosomal membranes using a filtration assay.
TBA
Targeting a uniquely nonspecific prenyl synthase with bisphosphonates to combat cryptosporidiosis.
University of Toronto
Structure-based dissection of the natural product cyclopentapeptide chitinase inhibitor argifin.
University of Dundee
The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases.
The Scripps Research Institute
Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.
Astex
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002.
Vertex Pharmaceuticals
SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa.
Bristol-Myers Squibb
Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.
Uppsala University
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.
Lawrence Berkeley National Laboratory
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.
Alcon Research
Carbonic anhydrase and matrix metalloproteinase inhibitors: sulfonylated amino acid hydroxamates with MMP inhibitory properties act as efficient inhibitors of CA isozymes I, II, and IV, and N-hydroxysulfonamides inhibit both these zinc enzymes.
Universita Degli Studi
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
Kochi Medical School
Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid.
Schering-Plough Research Institute
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.
Martin-Luther-University Halle-Wittenberg
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.
Faculte De Medecine Et De Pharmacie
Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.
Universitat Hamburg
8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors.
Wyeth-Ayerst Research
Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline.
Sankyo
Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.
Sunesis Pharmaceuticals
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.
Ciba-Geigy
INFLUENCE OF STEREOCHEMISTRY ON ACTIVITY AND BINDING MODES FOR C(2) SYMMETRY-BASED DIOL INHIBITORS OF HIV-1 PROTEASE.
Nci-Fcrdc
Thermodynamics of sequence-specific binding of PNA to DNA.
Chalmers University of Technology