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91 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28324649 99 Sulfonamides as Selective NaEBI Amgen Inc.
28287723 73 Sulfonamides as Selective NaEBI Amgen Inc.
28234467 108 Development of New Benzenesulfonamides As Potent and Selective NaEBI Bristol-Myers Squibb
28089699 63 Investigation of piperazine benzamides as human▀EBI Merck& Co. Inc.
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
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.
27994738 50 Sulfonamides as Selective NaEBI Amgen, Inc.
27080178 26 Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.EBI Gilead Sciences Inc.
27038498 33 Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.EBI Gilead Sciences Inc.
26985315 49 Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.EBI Xenon Pharmaceuticals, Inc.
26890998 572 Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx-1.EBI Amgen Inc.
26709102 142 Discovery of Vibegron: A Potent and Selective▀3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.EBI Merck Research Laboratories
26358159 114 Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.EBI Daiichi Sankyo Co., Ltd
26288685 59 Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI Merck Research Laboratories
25927480 36 Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.EBI Merck Research Laboratories
25288187 45 Bioavailable pyrrolo-benzo-1,4-diazines as Na(v)1.7 sodium channel blockers for the treatment of pain.EBI Merck Research Laboratory
25286150 75 Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.EBI AstraZeneca
26101568 51 Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.EBI Pfizer 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
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
25658507 218 Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.EBI Amgen Inc.
25113934 65 Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.EBI Merck Research Laboratory
25050166 58 Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.EBI Novartis Institutes for BioMedical Research
24937104 30 GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.EBI AstraZeneca
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
25176194 69 The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.EBI Xenon Pharmaceuticals Inc.
25155913 32 Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.EBI AstraZeneca
24601592 48 Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.EBI University College London
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
23121096 86 Ion channels as therapeutic targets: a drug discovery perspective.EBI Pfizer Inc.
21641215 55 Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship.EBI AstraZeneca
22770500 219 3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.EBI AstraZeneca
22708838 13 Lead optimization of antimalarial propafenone analogues.EBI St. Jude Children's Research Hospital
22939696 85 Phenethyl nicotinamides, a novel class of Na(V)1.7 channel blockers: structure and activity relationship.EBI AstraZeneca
22832315 85 Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.EBI AstraZeneca
24900334 89 N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.EBI TBA
22607672 28 MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.EBI Merck Research Laboratories
22191686 4 Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.EBI Universit£ degli Studi di Bari"Aldo Moro"
22318156 128 Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.EBI Amgen Inc.
22306122 90 The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.EBI Amgen Inc.
19645482 245 Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.EBI Merck Research Laboratories
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
18176998 45 Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.EBI Abbott Laboratories
17506538 27 Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.EBI Cardiome Pharma Corporation
7629795 13 4,5-Dihydro-3-(methanesulfonamidophenyl)-1-phenyl-1H-2,4-benzodiazepines: a novel class III antiarrhythmic agents.EBI Sterling Winthrop Research
22364743 8 Asymmetric synthesis and evaluation of a hydroxyphenylamide voltage-gated sodium channel blocker in human prostate cancer xenografts.EBI University of Virginia
22209205 38 Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.EBI Amgen Inc.
21955244 17 Optimization of propafenone analogues as antimalarial leads.EBI St. Jude Children's Research Hospital
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.
21634377 73 Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.EBI Amgen Inc.
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
21106456 35 Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.EBI Merck Research Laboratories
20855211 91 Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.EBI Abbott Laboratories
19682899 211 Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.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
19616432 176 Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.EBI Pfizer Global Research and Development
19500979 74 Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.EBI AstraZeneca R&D M£lndal
19481932 164 Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.EBI Merck Research Laboratories
18540666 8 Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.EBI Merck Research Laboratories
18529044 2 Sodium late current blockers in ischemia reperfusion: is the bullet magic?EBI Pierre Fabre Research Center
18501613 31 Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.EBI Abbott Laboratories
17489575 7 Sodium channel blockers.EBI Purdue Pharma L.P.
11720863 73 Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.EBI CeNeS Pharmaceuticals Inc.
28465103 22 Benzoxazolinone aryl sulfonamides as potent, selective NaEBI Merck& Co.
28389149 56 Discovery of selective, orally bioavailable, N-linked arylsulfonamide NaEBI Department of Discovery Chemistry Merck& Co.
28385504 52 The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.EBI WuXi AppTec (Shanghai) Co., Ltd.
19338333 37 Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.BDB Kochi Medical School
19138845 44 Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.BDB Merck Research Laboratories
16884309 5 Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.BDB TaiGen Biotechnology Co.
15993068 101 2-Aminoquinazoline inhibitors of cyclin-dependent kinases.BDB NAEJA Pharmaceutical Inc.
7932531 55 Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity.BDB SANDOZ Forschungsinstitut Ges.m.b.H.
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
11112523 7 Estimation of the hydrophobic effect in an antigen-antibody protein-protein interface.BDB University of Maryland Biotechnology Institute