Biological Activity of PF-04449913

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.
IC50 value: 5 nM [1]
Target: smoothened
PF-04449913, a Smoothened inhibitor was identified possessing excellent potency and physical properties that translate to an attractive predicted human pharmacokinetic profile. PF-04449913 was advanced to in vivo tumor growth inhibition studies, preclinical safety studies, and ultimately to human clinical trials. These results will be reported in separate disclosures.

References on PF-04449913

[1]. Michael J. Munchhof, et al. Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Med. Chem. Lett., 2012, 3 (2), pp 106–111