106 articles for thisTarget
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Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Glaxosmithkline
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with
Merck
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Merck Research Laboratories
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Merck
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Merck
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.
Gilead Sciences
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.
Gilead Sciences
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
Xenon Pharmaceuticals
Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx-1.
Amgen
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Merck Research Laboratories
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Daiichi Sankyo
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
Merck Research Laboratories
Bioavailable pyrrolo-benzo-1,4-diazines as Na(v)1.7 sodium channel blockers for the treatment of pain.
Merck Research Laboratory
Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.
Astrazeneca
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Pfizer
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Prediction of Thorough QT study results using action potential simulations based on ion channel screens.
University Of Oxford
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
University Of Oxford
Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.
Amgen
Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.
Merck Research Laboratory
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
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.
Astrazeneca
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.
Xenon Pharmaceuticals
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Astrazeneca
Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
University College London
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Merck
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.
Astrazeneca
Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship.
Astrazeneca
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Astrazeneca
Lead optimization of antimalarial propafenone analogues.
St. Jude Children'S Research Hospital
Phenethyl nicotinamides, a novel class of Na(V)1.7 channel blockers: structure and activity relationship.
Astrazeneca
Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.
Astrazeneca
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
TBA
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Merck Research Laboratories
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
Universit£
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.
Amgen
The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.
Amgen
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Merck Research Laboratories
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
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.
Abbott Laboratories
Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.
Cardiome Pharma
4,5-Dihydro-3-(methanesulfonamidophenyl)-1-phenyl-1H-2,4-benzodiazepines: a novel class III antiarrhythmic agents.
Sterling Winthrop Research
Asymmetric synthesis and evaluation of a hydroxyphenylamide voltage-gated sodium channel blocker in human prostate cancer xenografts.
University Of Virginia
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Amgen
Optimization of propafenone analogues as antimalarial leads.
St. Jude Children'S Research Hospital
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Merck
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Merck Frosst Centre For Therapeutic Research
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Merck Research Laboratories
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Abbott Laboratories
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
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.
Wyeth Research
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.
Pfizer
Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.
Astrazeneca R & D M£Lndal
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Merck Research Laboratories
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
Pierre Fabre Research Center
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Abbott Laboratories
Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.
Cenes Pharmaceuticals
Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).
Daiichi Sankyo
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na
Amgen
Discovery of non-zwitterionic aryl sulfonamides as Na
Bristol-Myers Squibb Research And Development
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid)
Sage Therapeutics
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na
Icagen
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
Vanderbilt University Institute Of Imaging Science
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Merck
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88
Astrazeneca
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na
Department Of Discovery Chemistry Merck
The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.
Wuxi Apptec (Shanghai)
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.
Merck Research Laboratories
Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.
Taigen Biotechnology
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity.
Sandoz Forschungsinstitut Ges.M.B.H.
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.
The Johns Hopkins University