PMID

Data

Article Title

Organization

Sulfonamides as Selective Na

Amgen

Sulfonamides as Selective Na

Amgen

[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.

TBA

Sulfonamides as Selective Na

Amgen

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

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

Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.

Pfizer

Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.

University of Oxford

Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.

University College London

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.

The Scripps Research Institute

Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.

Cambridge Neuroscience

 

Batrachotoxin binding site antagonists

TBA

Discovery of Selective Inhibitors of Na

Siteone Therapeutics

Discovery of Acyl-sulfonamide Na

Genentech

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

Discovery of DS-1971a, a Potent, Selective Na

Daiichi Sankyo

Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.

Amgen

Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na

Xenon Pharmaceuticals

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na

Genentech

The discovery and optimization of benzimidazoles as selective Na

Pfizer

Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na

Siteone Therapeutics

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

Anticonvulsant activity of piperidinol and (dialkylamino)alkanol esters.

TBA

Highly potent and selective Na

Pfizer

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

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

Yogi Vemana University

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University of Leipzig

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.