Table 1.

Clinically relevant synthetic Smo antagonists.

Compound	IC50 Wild-Type Smo	IC50 D473H Smo	Development Status	References
GDC-0449	3–22 nMa	Loss of activity	Clinically approved	[19–21]
NVP-LDE225	2.5 nM	Loss of activity	Phase III	[21,22]
PF-04449913	5 nM	ND	Phase II	[21,23]
BMS-833923	21 nM	ND	Phase II	[21,24]
LY2940680	2.4 nM	Activeb	Phase II	[21,25]

ND = Not determined or not reported

^aDependent on cellular assay

^bSpecific IC₅₀ values were not provided