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68 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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
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
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
24754640 28 New 5-unsubstituted dihydropyridines with improved CaV1.3 selectivity as potential neuroprotective agents against ischemic injury.EBI Universidad Complutense
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
10956198 2 Permanently charged chiral 1,4-dihydropyridines: molecular probes of L-type calcium channels. Synthesis and pharmacological characterization of methyl(omega-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate iodide, calcium channel antagonists.EBI State University of New York
8709127 29 Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.EBI Universit£ di Siena
7562902 114 Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.EBI SmithKline Beecham Pharmaceuticals
7837222 14 Calcium entry blockers and activators: conformational and structural determinants of dihydropyrimidine calcium channel modulators.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
8246246 13 A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels.EBI State University of New York
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
10522703 99 Design and synthesis of novel dihydropyridine alpha-1a antagonists.EBI Synaptic Pharmaceutical Corporation
21942426 113 Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.EBI Merck& Co.
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
 23 Heterocyclic guanidines as calcium antagonistsEBI 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
9784106 22 Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.EBI Chugai Pharmaceutical Company, Ltd.
8558529 195 Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.EBI Hoechst-Roussel Pharmaceuticals Inc.
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
7473567 7 Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.EBI Università di Siena
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 7 4-Isoxazolyl-1,4-dihydropyridines: biological, theoretical, and structural studies.EBI State University of New York
15131245 86 SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.BDB Sanofi-Synthelabo Recherche
12761331 97 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.BDB Case Western Reserve University
12721338 61 N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.BDB Pudue Pharma Discovery Research
12649361 779 L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.BDB Case Western Reserve University
12538838 14 Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.BDB Taisho Pharmaceutical Co.
11750180 139 Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.BDB Lilly Research Laboratories
11438309 51 The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.BDB Janssen Research Foundation
11082453 77 ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB Abbott Laboratories
9454810 72 SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.BDB Sanofi Recherche
8996185 121 Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.BDB Synthélabo Recherche
8935801 586 Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.BDB Janssen Research Foundation
8564266 77 Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.BDB Vrije Universiteit
7109844 11 The binding of [3H]nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats.BDB University of Arizona
3012067 36 (-)-[3H] desmethoxyverapamil labels multiple calcium channel modulator receptors in brain and skeletal muscle membranes: differentiation by temperature and dihydropyridines.BDB Johns Hopkins University
2338642 17 [3H]TA-3090, a selective benzothiazepine-type calcium channel receptor antagonist: in vitro characterization.BDB Marion Merrell Dow Inc.
1352553 38 Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist.BDB University of North Carolina