125 articles for thisTarget
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Article Title
Organization
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.
Goethe-University Frankfurt
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
Queen Mary University Of London
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Glaxosmithkline
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.
Abbvie
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.
Palacky University In Olomouc
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Merck Research Laboratories
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.
Vitae Pharmaceuticals
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
The University Of Tokyo
Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Bristol-Myers Squibb
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Merck Research Laboratories
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Merck Research Laboratories
Diethylstilbestrol-scaffold-based pregnane X receptor modulators.
University Of Ljubljana
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Merck Research Laboratories
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Bristol-Myers Squibb Research And Development
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Bristol-Myers Squibb R & D
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Bristol-Myers Squibb Research & Development
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.
Bristol-Myers Squibb Research
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Genentech
Discovery of novel pyrazole-containing benzamides as potent ROR¿ inverse agonists.
Biogen
Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.
Abbvie
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Identification of clinically used drugs that activate pregnane X receptors.
National Institutes Of Health Chemical Genomics Center
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
University Of Washington
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
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Genentech
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).
Genentech
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Merck Research Laboratories
Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.
Departments Of Discovery Chemistry, Metabolic Diseases, Lead Evaluation, Computer-Assisted Drug Design, Discovery Toxicology, Exploratory Clinical And Translational Research, And Pharmaceutical Candi
Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane X receptor antagonists.
University Of Ljubljana
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Bristol-Myers Squibb Research And Development
Insights on pregnane-X-receptor modulation. Natural and semisynthetic steroids from Theonella marine sponges.
Universit£
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
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Genentech
Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.
Merck Research Laboratories
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Merck Research Laboratories
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
City Of Hope National Medical Center
Synthesis and biological activity of pyridopyridazin-6-one p38a MAP kinase inhibitors. Part 2.
Merck Research Laboratories
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
Astrazeneca
Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.
TBA
Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.
Merck Research Laboratories
Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
TBA
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
University Of Michigan
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Merck Research Laboratories
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).
Westfalische Wilhelms-Universitat
Synthesis and biological evaluation of hyperforin analogues. Part I. Modification of the enolized cyclohexanedione moiety.
Universit£
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
Universit£
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
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
University Of Michigan
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
Total synthesis and pharmacological characterization of solomonsterol A, a potent marine pregnane-X-receptor agonist endowed with anti-inflammatory activity.
Universita Di Napoli Federico Ii
Substituted phenyl triazoles as selective inhibitors of 11 β-Hydroxysteroid Dehydrogenase Type 1.
Merck
Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity
TBA
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Merck Research Laboratories
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Merck Frosst Centre For Therapeutic Research
A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.
Merck Research Laboratories
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Merck Research Laboratories
Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.
Merck Research Laboratories
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.
Merck Research Laboratories
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
The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages.
Glaxosmithkline
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Bristol-Myers Squibb
Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).
Bristol-Myers Squibb Pharmaceutical Research And Development
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
Glaxosmithkline
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.
University Of Montpellier
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Glaxosmithkline
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Merck
Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.
Merck
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.
Bristol Myers Squibb
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Bristol-Myers Squibb Research And Development
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.
Merck
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against
Glaxosmithkline
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na
Xenon Pharmaceuticals
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Merck
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Bristol-Myers Squibb Research & Development
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
University Of Perugia
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute Of The Novartis Research Foundation (Gnf)
DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor.
University Of Maryland
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.
Bristol-Myers Squibb
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na
Bristol-Myers Squibb Research And Development
5-Substituted-N-pyridazinylbenzamides as potent and selective LRRK2 inhibitors: Improved brain unbound fraction enables efficacy.
Gsk Pharmaceuticals R&D
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
TBA
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Merck
Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists.
University Of Perugia
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists.
Bristol-Myers Squibb
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.
Bristol-Myers Squibb Research & Development
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia.
Merck
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD-1).
Bristol-Myers Squibb
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase.
Merck
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
Discovery of novel triazolobenzazepinones as ?-secretase modulators with central A?42 lowering in rodents and rhesus monkeys.
Merck Research Laboratories Boston
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
The University Of Tokyo
Alleviating CYP and hERG liabilities by structure optimization of dihydrofuran-fused tricyclic benzo[d]imidazole series - Potent, selective and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-2.
Glenmark Pharmaceuticals
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.
Glaxosmithkline
The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.
Bristol-Myers Squibb Research And Development
Discovery of BMS-961955, an allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Bristol-Myers Squibb Research And Development
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
Bristol-Myers Squibb Research And Development
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Merck
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11? hydroxysteroid dehydrogenase type 1 inhibitor.
Vitae Pharmaceuticals
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Merck
Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.
Metabasis Therapeutics
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na
Department Of Discovery Chemistry Merck
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
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
