Fluorescent probes for use in protein kinase inhibitor binding assay

摘要

The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The K_d for the inhibitor compound is derived based on the K_d of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides novel active site probes suitable for use with the screening method.