175 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
Lactam-stabilized helical analogues of the analgesicµ-conotoxin KIIIA.
Monash University
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
Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.
University of Utah
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
Development of Riluzole Analogs with Improved Use-Dependent Inhibition of Skeletal Muscle Sodium Channels.
University of Bari Aldo Moro
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (Na
Xenon Pharmaceuticals
Design, synthesis, and biological evaluation of acyl sulfonamide derivatives with spiro cycles as Na
Fudan University
Recent encounters with atropisomerism in drug discovery.
Bristol-Myers Squibb Research and Development
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 α 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 β-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
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
Siteone Therapeutics
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
Benzopyrroloxazines containing a bridgehead nitrogen atom as promising scaffolds for the achievement of biologically active agents.
University of Calabria
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)
HETEROCYCLIC COMPOUND, AND INTERMEDIATE THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF
Wuhan LL Science and Technology Development Co.
Iminosulfanone compound as bromodomain protein inhibitor and pharmaceutical composition and medical use thereof
Chia Tai Tianqing Pharmaceutical Group
Pentafluorosulfanyl-substituted amide derivatives, preparation methods thereof and medical uses thereof
Beijing Innocare Pharma Tech
Vasopressin receptor antagonists and products and methods related thereto
Blackthorn Therapeutics
Composition for inducing differentiation and protection of neural stem cells and method for inducing neuro-regeneration using the same composition
Genuv
3-((hetero-)aryl)-alkyl-8-amino-2-oxo-l,3-diaza-spiro-[4.5]-decane derivatives
Gruenenthal
Pyrimidine derivative, method for preparing same and use thereof in medicine
Zhejiang Hisun Pharmaceutical
5-oxa-2-azabicyclo[2.2.2]OCTAN-4-yl and 5-oxa-2-azabicyclo[2.2.1]heptan-4-yl derivatives
Hoffmann-La Roche
Two amino acid residues confer different binding affinities of Abelson family kinase SRC homology 2 domains for phosphorylated cortactin.
Yale University
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.
University of Cambridge
Tetrahydroacridine derivatives with fluorobenzoic acid moiety as multifunctional agents for Alzheimer's disease treatment.
Medical University of Lodz
An Unusual Protector-Protégé Strategy for the Biosynthesis of Purine Nucleoside Antibiotics.
Wuhan University
Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities
Almirall
Substituted 3-haloallylamine inhibitors of ASSAO and uses thereof
Boehringer Ingelheim International
Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
Pharmacyclics
Characterization of MymA protein as a flavin-containing monooxygenase and as a target of isoniazid.
Miranda House
3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.
Jilin University
Rational design and synthesis of dihydropyrimidine based dual binding site acetylcholinesterase inhibitors.
Hazara University
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.
Genentech
Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.
Birla Institute of Technology
Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
Sanofi
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.
University of Wisconsin-Madison
Indanyl-substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-C]pyridines, their use as medicament, and pharmaceutical preparations comprising them
Sanofi
Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy
Pantarhei Bioscience
Naphthyridine derivatives as inhibitors of hypoxia inducible factor (HIF) hydroxylase
Fibrogen
1,3-disubstituted-4-aminopyrazolo [3, 4-d] pyrimidines, a new class of potent inhibitors for phospholipase D.
University of Massachusetts Boston
Kinetic and thermodynamic rationale for suberoylanilide hydroxamic acid being a preferential human histone deacetylase 8 inhibitor as compared to the structurally similar ligand, trichostatin a.
North Dakota State University
6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands
Rottapharm
Novel Inhibitor Binding Site Discovery on HIV-1 Capsid N-Terminal Domain by NMR and X-ray Crystallography.
Boehringer Ingelheim (Canada)
Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.
I.G.B.M.C.
Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.
Case Western Reserve University
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.
Case Western Reserve University
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.
The Royal Danish School of Pharmacy
Synthetic modification of prostaglandin f(2alpha) indicates different structural determinants for binding to the prostaglandin F receptor versus the prostaglandin transporter.
Albert Einstein College of Medicine
Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors.
Cocensys
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.
Eli Lilly
I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor.
Neurogen
Synthesis, kinetic evaluation and cell-based analysis of C-alkylated isofagomines as chaperones of β-glucocerebrosidase.
University of British Columbia
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
Abbott Laboratories
An alternative purification method for human serum paraoxonase 1 and its interactions with sulfonamides.
Ataturk University
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma