CID 2011756 is an ATP-competitive PKD1 inhibitor, with an IC 50 of 3.2 µM. CID 2011756 decreases the phosphorylation of endogenous PKD1 Ser 916 in LNCaP cancer cells with an EC 50 of 10±0.7 µM. CID 2011756 also has cellular pan-PKD inhibitory effects, with IC 50 s of 0.6±0.1 µM and 0.7±0.2 µM for PKD2 and PKD3, respectively.