Journal
ACTA PHARMACOLOGICA SINICA
Volume 37, Issue 1, Pages 34-43Publisher
ACTA PHARMACOLOGICA SINICA
DOI: 10.1038/aps.2015.108
Keywords
ion channels; high throughput screening; ligand binding assay; flux-based assay; fluorescence-based assay; automated electrophysiological assay; drug discovery
Funding
- National Natural Sciences Foundation of China [81470163, 81503056]
- National Major Special Project on New Drug Innovation of China [2014ZX09507003-006-008]
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Ion channels are involved in a variety of fundamental physiological processes, and their malfunction causes numerous human diseases. Therefore, ion channels represent a class of attractive drug targets and a class of important off-targets for in vitro pharmacological profiling. In the past decades, the rapid progress in developing functional assays and instrumentation has enabled high throughput screening (HTS) campaigns on an expanding list of channel types. Chronologically, HTS methods for ion channels include the ligand binding assay, flux-based assay, fluorescence-based assay, and automated electrophysiological assay. In this review we summarize the current HTS technologies for different ion channel classes and their applications.
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