Purmorphamine is an activator of Smoothened, and blocks BODIPY-cyclopamine binding to Smo with IC50 of appr 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

PF 5274857 HCl is a high affinity and selective Smoothened (Smo) receptor antagonist with Ki of 4.6 nM.

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.

PF-04449913 is a potent and orally bioavailable smoothened inhibitor. PF-04449913 binds to human SMO (amino acids 181-787) with an IC50 of 4 nM.

Inhibitor of Hedgehog (Hh) signaling; antagonizes smoothened activity

LDE225 diphosphate is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.

IHR 1 is a potent Smo antagonist with IC50 of 7.6 nM.

LDE225 is an antagonist of Smoothened that can inhibit hedgehog signaling with IC50 of 2.5 nM.

Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

BMS-833923 is an inhibitor of Smoothened with potential antineoplastic activity. It can also inhibit BODIPY cyclopamine binding to SMO with IC50 of 21 nM.

SAG HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

Jervine is hedgehog signaling inhibitor with IC50 of 500 nM-700 nM that disrupts the interaction with smoothened.