161 articles for thisTarget
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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
Nav1.7 Inhibitors: Potential Effective Therapy for the Treatment of Chronic Pain.
Therachem Research Medilab (India)
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Daiichi Sankyo
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
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Pfizer
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
Studies examining the relationship between the chemical structure of protoxin II and its activity on voltage gated sodium channels.
Purdue Pharma
The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.
Xenon Pharmaceuticals
Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
University College London
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
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
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
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Imidazopyridines: a novel class of hNav1.7 channel blockers.
Merck Research Laboratories
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
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain.
Xenon Pharmaceuticals
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Merck Research Laboratories
Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.
Merck Research Laboratories
Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.
University of North Carolina
Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain.
Merck Research Laboratories
Discovery of a novel class of isoxazoline voltage gated sodium channel blockers.
Merck Research Laboratories
3-Amino-1,5-benzodiazepinones: potent, state-dependent sodium channel blockers with anti-epileptic activity.
Merck Research Laboratories
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Merck Research Laboratories
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
Merck Research Laboratories
Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.
Merck Research Laboratories
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Merck Research Laboratories
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Merck Research Laboratories
Functional Characterization of the Nemertide ? Family of Peptide Toxins.
Uppsala University
Identification of aryl sulfonamides as novel and potent inhibitors of Na
Xenon Pharmaceuticals
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I
Gilead Sciences
Exploration of TRPM8 Binding Sites by ?-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities.
University of Salerno
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
Amgen
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na
Bristol-Myers Squibb Research and Development
Discovery of new indole-based acylsulfonamide Na
Bristol-Myers Squibb Research and Development
Substituted 4-phenyl-2-aminoimidazoles and 4-phenyl-4,5-dihydro-2-aminoimidazoles as voltage-gated sodium channel modulators.
University of Ljubljana
Novel state-dependent voltage-gated sodium channel modulators, based on marine alkaloids from Agelas sponges.
University of Ljubljana
A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain.
Merck Research Laboratories
QSAR investigation of NaV1.7 active compounds using the SVM/Signature approach and the Bioclipse Modeling platform.
Astrazeneca
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa
Xenon Pharmaceuticals
Discovery of morpholine-based aryl sulfonamides as Na
Bristol-Myers Squibb Research and Development
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Idorsia Pharmaceuticals
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
Wuxi Apptec (Shanghai)
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
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 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)
Trace amines: identification of a family of mammalian G protein-coupled receptors.
Synaptic Pharmaceutical
6-(N-benzoylamino)purine as a novel and potent inhibitor of xanthine oxidase: inhibition mechanism and molecular modeling studies.
National Institute of Pharmaceutical Education and Research
Characterisation of the melanocortin 4 receptor by radioligand binding.
Uppsala University
Impact of linker strain and flexibility in the design of a fragment-based inhibitor.
Johns Hopkins University
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
Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct.
Universita Degli Studi Di Firenze
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
Quorex Pharmaceuticals
Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism.
Novartis
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
University of Alberta
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.
Eli Lilly
Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.
Taigen Biotechnology
Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands.
Merck Research Laboratories
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.
Abbott Bioresearch Center
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
University of Pennsylvania
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.
Merck Research Laboratories