Predictor hERG Fluorescence Polarization Assay Kit Performed on the PHERAstar Plus

The potential for cardiotoxic side-effects continues to challenge the development of small molecule based therapies. These intolerable side-effects are often precipitated by drug-induced long QT syndrome (LQT), which is often linked to blocking the human ether-a-go-go related gene (hERG) potassium channel.

Although patch-clamp electrophysiology remains the gold standard for determining the interaction of compounds with the function of the hERG channel, radioligand displacement assays have proven to be a cost-effective initial alternative assay for hERG channel liability at early stages of compound development. Speed and cost still suffer however, as radioligand displacement assays remain heterogeneous and depend on the procurement and disposal costs of radioligands. Because the FDA has recommended that all new drug candidates be tested for blockage of the hERG channel, there is a pressing need for a simple, safe, cost-effective method to triage compounds earlier in the discovery process.