Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310
Published 2021 View Full Article
- Home
- Publications
- Publication Search
- Publication Details
Title
Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310
Authors
Keywords
-
Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume -, Issue -, Pages -
Publisher
American Chemical Society (ACS)
Online
2021-03-08
DOI
10.1021/acs.jmedchem.1c00049
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- Practical Early Development Synthesis of Nav1.7 Inhibitor GDC-0310
- (2020) Andreas Stumpf et al. SYNTHESIS-STUTTGART
- Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain
- (2019) Steven J. McKerrall et al. JOURNAL OF MEDICINAL CHEMISTRY
- Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study in Healthy Volunteers
- (2019) Michael E. Rothenberg et al. CLINICAL DRUG INVESTIGATION
- Improved Synthesis of the Nav1.7 Inhibitor GDC-0276 via a Highly Regioselective SNAr Reaction
- (2019) Andreas Stumpf et al. ORGANIC PROCESS RESEARCH & DEVELOPMENT
- Nav1.7 inhibitors for the treatment of chronic pain
- (2018) Steven J. McKerrall et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain
- (2018) Girish Bankar et al. Cell Reports
- Prevalence of Chronic Pain and High-Impact Chronic Pain Among Adults — United States, 2016
- (2018) James Dahlhamer et al. MMWR-MORBIDITY AND MORTALITY WEEKLY REPORT
- Identification of Selective Acyl Sulfonamide–Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity
- (2018) Shaoyi Sun et al. JOURNAL OF MEDICINAL CHEMISTRY
- Insensitivity to Pain upon Adult-Onset Deletion of Nav1.7 or Its Blockade with Selective Inhibitors
- (2018) Shannon D. Shields et al. JOURNAL OF NEUROSCIENCE
- 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 NaV1.7
- (2017) Nigel. A. Swain et al. JOURNAL OF MEDICINAL CHEMISTRY
- Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
- (2017) Matthew M. Weiss et al. JOURNAL OF MEDICINAL CHEMISTRY
- Effect of Chirality on Common in Vitro Experiments: An Enantiomeric Pair Analysis
- (2015) Jeffrey T. Bagdanoff et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist
- (2015) S. Ahuja et al. SCIENCE
- Recent progress in sodium channel modulators for pain
- (2014) Sharan K. Bagal et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Global Nav1.7 Knockout Mice Recapitulate the Phenotype of Human Congenital Indifference to Pain
- (2014) Jacinthe Gingras et al. PLoS One
- A Novel Method for High Throughput Lipophilicity Determination by Microscale Shake Flask and Liquid Chromatography Tandem Mass Spectrometry
- (2013) Baiwei Lin et al. COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
- Inherited Cardiac Diseases Caused by Mutations in the Nav1.5 Sodium Channel
- (2009) JACOB TFELT-HANSEN et al. JOURNAL OF CARDIOVASCULAR ELECTROPHYSIOLOGY
- Inherited Neuronal Ion Channelopathies: New Windows on Complex Neurological Diseases
- (2008) W. A. Catterall et al. JOURNAL OF NEUROSCIENCE
Become a Peeref-certified reviewer
The Peeref Institute provides free reviewer training that teaches the core competencies of the academic peer review process.
Get StartedAsk a Question. Answer a Question.
Quickly pose questions to the entire community. Debate answers and get clarity on the most important issues facing researchers.
Get Started