84 articles for thisTarget

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The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
28252961	13	Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.	Goethe-University Frankfurt
28151659	89	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
28523109	79	Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.	Glaxosmithkline
28185720	42	Discovery of phenyl acetamides as potent and selective GPR119 agonists.	Merck
27994765	95	Discovery of Highly Potent Liver X Receptorß Agonists.	Bristol-Myers Squibb
27077528	4	Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.	Abbvie
27145071	37	2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.	Palacky University In Olomouc
27190600	48	Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.	Merck Research Laboratories
26990539	79	Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.	Vitae Pharmaceuticals
26905831	11	Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.	The University Of Tokyo
26917221	69	Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.	Bristol-Myers Squibb
26850003	1	Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.	Merck Research Laboratories
26709102	142	Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.	Merck Research Laboratories
26408814	5	Diethylstilbestrol-scaffold-based pregnane X receptor modulators.	University Of Ljubljana
26288697	41	Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.	Merck Research Laboratories
26288692	37	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.	Bristol-Myers Squibb Research And Development
26288683	43	Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.	Bristol-Myers Squibb R & D
26321361	56	Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.	Genentech
26288682	64	Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.	Bristol-Myers Squibb Research & Development
26191364	10	Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.	Bristol-Myers Squibb Research
26048793	91	Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.	Genentech
26048789	143	Discovery of novel pyrazole-containing benzamides as potent ROR¿ inverse agonists.	Biogen
26101566	14	Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.	Abbvie
26005524	147	Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.	Merck Research Laboratories
20966043	200	Identification of clinically used drugs that activate pregnane X receptors.	National Institutes Of Health Chemical Genomics Center
22679214	13	Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.	University Of Washington
25101488	50	Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.	Bristol-Myers Squibb
25050169	52	Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11ß-Hydroxysteroid Dehydrogenase Type 1 (11ß-HSD-1).	Bristol-Myers Squibb
25017032	62	Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.	Genentech
24502334	123	Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).	Genentech
25453817	130	A reversed sulfonamide series of selective RORc inverse agonists.	Argenta Discovery
25305688	41	Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.	Phenex Pharmaceuticals
25248679	85	Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.	Merck Research Laboratories
25208139	40	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
24828006	4	Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane X receptor antagonists.	University Of Ljubljana
24397558	45	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
24388834	3	Insights on pregnane-X-receptor modulation. Natural and semisynthetic steroids from Theonella marine sponges.	Universit£
24360604	60	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
24239186	84	Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.	Genentech
24900606	12	Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.	Merck Research Laboratories
24157366	46	Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.	Merck Research Laboratories
23707259	98	The discovery of BMS-457, a potent and selective CCR1 antagonist.	Bristol-Myers Squibb
23688559	30	Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.	City Of Hope National Medical Center
22901390	44	Synthesis and biological activity of pyridopyridazin-6-one p38a MAP kinase inhibitors. Part 2.	Merck Research Laboratories
21907579	22	Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.	Astrazeneca
24900283	80	Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.	TBA
23098566	17	Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.	Merck Research Laboratories
24900461	49	Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.	TBA
22452568	2	Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.	University Of Michigan
22364528	412	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
20408551	13	Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).	Westfalische Wilhelms-Universitat
20188553	66	Tetrahydroindolizinone NK1 antagonists.	Merck Research Laboratories
11975475	1	Synthesis and biological evaluation of hyperforin analogues. Part I. Modification of the enolized cyclohexanedione moiety.	Universit£
16250653	22	Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.	Universit£
21983439	65	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
21903392	11	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
21689935	55	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
21599020	2	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
21334894	218	Substituted phenyl triazoles as selective inhibitors of 11 β-Hydroxysteroid Dehydrogenase Type 1.	Merck
24900253	28	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity	TBA
21147532	82	Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.	Merck Research Laboratories
21106375	198	Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.	Merck Frosst Centre For Therapeutic Research
21195616	26	A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.	Merck Research Laboratories
21106456	35	Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.	Merck Research Laboratories
20729082	59	Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.	Merck Research Laboratories
20709545	31	Substituted biaryl pyrazoles as sodium channel blockers.	Merck Research Laboratories
20638278	145	Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.	Phenex Pharmaceuticals
20378346	25	Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.	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
19717304	29	The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages.	Glaxosmithkline
19541481	57	Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.	Bristol-Myers Squibb
19419866	24	Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).	Bristol-Myers Squibb Pharmaceutical Research And Development
18800767	45	Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.	Glaxosmithkline
18440811	207	4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.	Merck Research Laboratories
18304819	34	N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.	University Of Montpellier
16529931	139	SAR studies: designing potent and selective LXR agonists.	Merck Research Laboratories
16451063	139	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
29035567	38	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
28389149	56	Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na	Department Of Discovery Chemistry Merck
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