Figure 1.

Pipeline of high-throughput screening targeting ion channels. (A) For a large compound library, the compounds are first screened using the fluorescence-based flux assay on an ion channel-expressed stable cell line, and the identified hits are confirmed on the same cells and are counter-screened on the parental cells to exclude non-specific hits. (B) Second, active hits are tested using an automated patch clamp for validation and, the active hits are pharmacologically evaluated for structure-activity relationship (SAR) until lead compounds are identified. (C) Finally, a manual patch clamp is used to characterize biophysical properties on stable cell lines and native cells.