Assay Detail
Binding
CHEMBL2045142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed as effect on SMO/SHH transient transcriptional activation after 20 hrs by Gli-luciferase reporter assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | C3H 10T1/2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.58 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2043430 | — | — | 1 | 8.30 |
| CHEMBL2043435 | — | — | 1 | 8.30 |
| CHEMBL2043437 | GLASDEGIB | 4.0 | 1 | 8.30 |
| CHEMBL473417 | VISMODEGIB | 4.0 | 1 | 8.30 |
| CHEMBL2043436 | — | — | 1 | 7.70 |
| CHEMBL2043434 | — | — | 1 | 7.46 |
| CHEMBL2043432 | — | — | 1 | 7.37 |
| CHEMBL2043433 | — | — | 1 | 7.35 |
| CHEMBL2043438 | — | — | 1 | 7.14 |
| CHEMBL2043431 | — | — | 1 | 7.06 |
| CHEMBL2043429 | — | — | 1 | 6.99 |
| CHEMBL2043439 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2043430 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2043435 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2043437 | GLASDEGIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL473417 | VISMODEGIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2043436 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2043434 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2043432 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2043433 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2043438 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2043431 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2043429 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2043439 | — | IC50 | = | 191.0 | nM | 6.72 |