KAT2B and cancer: Compound 3 (reference compound 14) showed moderate binding activity using Isothermal Titration Calorimetry (ITC) (PCAF KD 6.80 μM, Fig. 2).30 More recently Genentech and Constellation pharmaceuticals disclosed the structures of highly potent compounds 4, 5 and 6 (reference examples 20, 65B and 18 respectively) (IC50 19 nM and 70 nM respectively, Fig. 2) for the treatment of PCAF mediated diseases including cancer.21,22,31