title: Ion channel profiling to advance drug discovery and development.
abstract: In vitro pharmacological profiling provides crucial information to eliminate drug candidates with potential toxicity early in drug discovery and reduce failure in later stages. It has become a common practice in industry to test lead compounds against a panel of ion channel targets for selectivity and safety liability at early drug discovery stages. Ion channel profiling technologies include binding assays, flux assays, fluorescent membrane potential assays, automated and conventional electrophysiology. Instead of examining compound effects on individual ion channel targets, automated current clamp, optical electrophysiology, and multi-electrode assays have evolved to investigate the integrated compound effects on cardiac myocytes. This review aims to provide an overview of ion channel profiling for cardiac safety and comparisons of various technologies.
authors.affiliation: Molecular Devices LLC, 1311 Orleans Drive, Sunnyvale, CA 94089, United States. Electronic address: beiyan.zou@moldev.com.
authors.forename: Beiyan
authors.initials: B
authors.lastname: Zou
mesh_terms: D000818:Animals; D001145:Arrhythmias, Cardiac / Q000139:chemically induced* / Q000378:metabolism; D001681:Biological Assay; D002478:Cells, Cultured; D055808:Drug Discovery / Q000379:methods*; D015507:Drugs, Investigational / Q000633:toxicity*; D006801:Humans; D007473:Ion Channels / Q000378:metabolism*; D008564:Membrane Potentials / Q000187:drug effects; D032383:Myocytes, Cardiac / Q000187:drug effects* / Q000378:metabolism; D018408:Patch-Clamp Techniques; D011485:Protein Binding; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D015507:Drugs, Investigational; D007473:Ion Channels