TP-238 hydrochloride is a highly potent and selective dual CECR2/BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases.

CECR2:7.5 (pIC50), CECR2:30 nM, CECR2:10 nM (Kd), BPTF:120 nM (Kd), BPTF:6.5 (pIC50), BPTF:350 nM, BRD9:5.9 (pIC50)

TP-238 has on target biochemical activity of 10-30 nM with CECR2 and 100-350 nM with BPTF. TP-238 displays potency for both CECR2 (pIC50 of 7.5) and BPTF (pIC50 of 6.5) in an Alpha screen assay. Isothermal titration calorimetry (ITC) shows TP-238 with a Kd of 10 nM for CECR2 and 120 nM for BPTF[1][2].