| S7092 |
SANT-1 |
SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM. |
Selective |
Smoothened receptor, Kd: 1.2 nM |
| S2151 |
LDE225 (NVP-LDE225,Erismodegib) |
LDE225 (NVP-LDE225,Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. Phase 3. |
Selective |
Smo (human), IC50: 2.5 nM; Smo (mouse), IC50: 1.3 nM |
| S2777 |
PF-5274857 |
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. |
Selective |
Smoothened, Ki: 4.6 nM; Smoothened, IC50: 5.8 nM |
| S7160 |
Glasdegib (PF-04449913) |
Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
|
Selective |
Smoothened, IC50: 5 nM |
| S1146 |
Cyclopamine |
Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM. |
Selective |
Smoothened, IC50: 46 nM |
| S3042 |
Purmorphamine |
Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM. |
Selective |
Smoothened, IC50: ~1.5 μM |
| S7138 |
BMS-833923 |
BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2. |
Selective |
|
| S2157 |
Taladegib (LY2940680) |
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. |
Selective |
|
