In Vitro Potency Assessment of hERG Inhibitors: Cell-Based Thallium-Sensitive Fluorescence Assay vs. Automated Electrophysiology

The human ether-á-go-go related gene (hERG) encodes a voltage-gated potassium channel, which plays a critical role in the repolarization of the cardiac action potential. This study shows the optimization and validation of a robust cell-based hERG fluorescence assay on the FLIPR Tetra® Instrument. This method has been shown to have the throughput capability for early stage in vitro hERG assessment and the accuracy of potency assessment comparable to that obtained by electrophysiological recording techniques.