Determination of Drug-Kinase Residence Time with the Transcreener® ADP2 FP Assay
2 September 2015
This application note provides a protocol and experimental example for the use of the Transcreener® ADP2 FP Assay 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. This in turn allows longer pharmacological reducing off-target effects.