Determination of Drug-Kinase Residence Time with the Transcreener® ADP2 FP Assay

This application note provides a protocol and experimental example for the use of the Transcreener® ADP2 FP Assay from BellBrook Labs to determine the residence time of a drug (or drug candidate) during its interaction with a kinase. The duration of residence time may be highly relevant for assessing the durable pharmacologic effects of a drug candidate. In general, longer residence time results in improved efficacy, as the extended contact between drug and enzyme results in extended inhibition of enzyme activity which in turn allows longer pharmacological effects at lower doses reducing off-target effects.