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50 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28254166 81 Discovery of novel BTK inhibitors with carboxylic acids.EBI Merck & Co Inc
28523109 79 Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.EBI GlaxoSmithKline
2391701 26 Dihydropyrimidine calcium channel blockers. 2. 3-substituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.EBI Squibb Institute for Medical Research
2840498 10 Dimeric 1,4-dihydropyridines as calcium channel antagonists.EBI State University of New York
3339603 9 Crystal structures and pharmacologic activities of 1,4-dihydropyridine calcium channel antagonists of the isobutyl methyl 2,6-dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (nisoldipine) series.EBI University of Oslo
27939174 84 Challenges in the development of an MEBI Vanderbilt University Medical Center
28105282 95 Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 withEBI Merck& Co.
27839686 65 Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.EBI Merck Research Laboratories
27815121 132 Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.EBI Merck& Co.
27994747 66 Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.EBI Merck& Co.
27579577 91 Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.EBI Actelion Pharmaceuticals Ltd.
26709102 142 Discovery of Vibegron: A Potent and Selective▀3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.EBI Merck Research Laboratories
26288685 59 Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI Merck Research Laboratories
26231163 50 Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.EBI Actelion Pharmaceuticals Ltd
25286150 75 Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.EBI AstraZeneca
26101566 14 Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.EBI AbbVie, Inc.
26005536 92 Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI Merck Research Laboratories
26005524 147 Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.EBI Merck Research Laboratories
22761000 123 Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.EBI Jagiellonian University
25087753 240 Prediction of Thorough QT study results using action potential simulations based on ion channel screens.EBI University of Oxford
21300721 90 Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.EBI University of Oxford
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
25155913 32 Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.EBI AstraZeneca
24660890 12 Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.EBI Merck & Co., Inc.
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
23098566 17 Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.EBI Merck Research Laboratories
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.EBI Merck Research Laboratories
22607672 28 MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.EBI Merck Research Laboratories
19645482 245 Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.EBI Merck Research Laboratories
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI F-59000 Lille
7837222 14 Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
2329573 8 Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.EBI Princ
2435904 12 Diethyl 3,6-dihydro-2,4-dimethyl-2,6-methano-1,3-benzothiazocine-5,11- dicarboxylates as calcium entry antagonists: new conformationally restrained analogues of Hantzsch 1,4-dihydropyridines related to nitrendipine as probes for receptor-site conformation.EBI TBA
21621998 110 Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.EBI Merck Frosst Centre for Therapeutic Research
21514824 91 3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.EBI Merck Research Laboratories
21257308 28 High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.EBI Merck Research Laboratories
21316226 12 Pyridyl amides as potent inhibitors of T-type calcium channels.EBI Merck Research Laboratories
19888755 43 Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.EBI Wyeth Research
 3 4-Biaryl-substituted dihydropyridines with an unusual antiperiplanar conformationEBI TBA
 15 Phenyl-glycinol based NK1 receptor antagonists — towards the minimum pharmacophoreEBI TBA
19481932 164 Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.EBI Merck Research Laboratories
18817368 57 Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI Merck Research Laboratories
17588748 46 Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.EBI Merck Research Laboratories
10447952 16 Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships.EBI State University of New York
8474099 3 Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile.EBI Università di Firenze
2435903 4 Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters.EBI TBA
2142737 14 4-Isoxazolyl-1,4-dihydropyridines: biological, theoretical, and structural studies.EBI State University of New York
26833890 18 Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.BDB Yogi Vemana University
26469307 7 Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB University of Leipzig
12534275 32 A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.BDB The Johns Hopkins University