TABLE 3.
Potency of Smo modulators using [3H]MRT-92 binding to human WT Smo and D473H6.54f mutant receptors
| Compound |
Ki (nM) |
|
|---|---|---|
| WT | D473H6.54f | |
| MRT-92 | 0.7 ± 0.1 | 0.7 ± 0.2 |
| MRT-83 | 4.6 ± 0.7 | 5.5 ± 0.2 |
| ALLO-2 | 3.8 ± 1.5 | 5.1 ± 2.0 |
| LDE225 | 1.6 ± 0.4 | 108 ± 18*** |
| GDC-0449 | 5.8 ± 1.3 | >1000*** |
| LY2940680 | 0.5 ± 0.2 | 55 ± 0.8*** |
| SANT-1 | 1.1 ± 0.1 | 67 ± 0.9*** |
| M25 | 0.9 ± 0.1 | 61 ± 13*** |
| Itraconazole | 28.3 ± 0.1 | >1000*** |
| SAG | 2.4 ± 0.3 | 45 ± 0.3*** |
| Purmorphamine | >5000 | ND |
Data (means ± sem of 3 to 5 independent experiments) derived from experiments, as shown in Supplemental Fig. 4. ND, not determined.
***
P ≤ 0.001.