Protein Binding-dependent Decreases in hERG Channel Blocker Potency Assessed by Whole-Cell Voltage Clamp in Serum

Abstract:In vitro hERG blocking potency is measured in drug discovery as part of an integrated cardiovascular risk assessment. Typically, the concentrations producing 50% inhibition are measured in protein-free saline solutions and compared with calculated free therapeutic in vivo Cmax values to est