Figure 1.

Dasatinib and JQ-1-derived photoaffinity probes containing 2-aryl-5-carboxy-tetrazole (ACT), diazirine (DA), or benzophenone (BP) photoaffinity label (PAL) and their biological activities. (a) Structures of the photoaffinity probes. (b) Kinome profiling of Dasatinib-derived photoaffinity probes. A panel of 82 protein kinases were surveyed in this assay, and inhibition constants, K_i, are given in micromolar. See Table S1 in the Supporting Information for K_i values. The nonreceptor tyrosine kinase targets are indicated by blue arrows. NV, no value. (c) Plots of the inhibition of BRD-2, -3, and -4 by JQ-1-derived photoaffinity probes. See Table S2 in the Supporting Information for K_i values.