Test
The best known kinase inhibitor, Gleevec (Imatinib), binds a non-activated form of Abl. Such inhibitors are therefore more difficult to detect using activity based assays, so it is worthwhile to set up kinase binding assays for your kinase of interest in order to avoid missing out on such compounds. Moreover the HTRF kinase binding assays are easily set up, using a mix and measure detection format in the absence of ATP. Direct displacement of the fluorescent-inhibitor from the ATP binding pocket is measured, enabling the determination of the affinity of your inhibitor by performing dose response curves. Purified kinase preparation is less critical compared to enzymatic assays, since measurements can be performed on kinases which have little or no activity.