PMID

Data

Article Title

Organization

Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.

University of Kansas Specialized Chemistry Center

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.

Vanderbilt University Medical Center

3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.

Astrazeneca

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.

Vanderbilt University Medical Center

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

Bristol-Myers Squibb Pharmaceutical Research Institute

General Pharmacological Activation Mechanism of K

East China Normal University

Discovery, synthesis and biological characterization of a series of

University of Nebraska

Development of an automated screen for Kv7.2 potassium channels and discovery of a new agonist chemotype.

University of Michigan

An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.

Marquette University

Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.

University Federico Ii of Naples

Kv7 (KCNQ) channel modulators and neuropathic pain.

Neurosearch

Design, synthesis and evaluation of novel N-phenylbutanamide derivatives as KCNQ openers for the treatment of epilepsy.

Nanjing University of Technology

Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents.

Nanjing University of Technology