Figure 1 from Drug–Drug Interaction Liabilities with BTK Inhibitor TL-895

Interaction of TL-895 with protein kinases. A, KINOMEscan of TL-895 (500 nmol/L) against 403 nonmutant kinases to determine a selectivity score S(35) of 0.015. B, Kinase profiling of TL-895 against BTK and BMX revealed EC₅₀ values of 3.02 and 0.53 nmol/L, respectively. Data represent the mean values (symbols) and SD (error bars) of two independent experiments performed in duplicate. C, Bioluminescence resonance energy transfer (BRET) luciferase response of BTK and BMX in the presence of TL-895 in HEK293 cells expressing BTK- and BMX-NanoLuc Fusion Vector showing EC₅₀ values of 6.8 and 1.6 nmol/L, respectively. Data represent mean values (symbols) and SD (error bars) of two independent experiments performed in duplicate.