HTS assays for developing the molecular pharmacology of ion channels

•Improved ion channel assay technologies have become available over the past ten years.•Fluorescent assay methods are most common in ion channel HTS.•High throughput electrophysiology may become alternative approach for focused libraries.•Improvements in sensor technologies will drive advances in ion channel discovery.

Ion channels remain important targets for drug discovery. Improvements in ion channel screening technologies over the past ten years have provided opportunities for drug discovery on novel and known targets by enabling efficient, high throughput screening and improved compound profiling. Fluorescent assays using ion-specific or membrane potential sensors are the most commonly used methods in high throughput campaigns due to a favorable combination of throughput, cost and information content. Automated electrophysiology instruments provide a valuable complement to fluorescent assays for many channel types and are emerging as alternative approaches for high throughput screening.