Assay Detail
Binding
CHEMBL2162705
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Displacement of [3H]cyclopamine from wild type Smo expressed in U2OS cells after 2 hrs by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.83 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105737 | SONIDEGIB | 4.0 | 1 | 8.22 |
| CHEMBL254129 | CYCLOPAMINE | — | 1 | 7.90 |
| CHEMBL473417 | VISMODEGIB | 4.0 | 1 | 7.79 |
| CHEMBL2160208 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105737 | SONIDEGIB | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL254129 | CYCLOPAMINE | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL473417 | VISMODEGIB | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL2160208 | — | Ki | = | 37.9 | nM | 7.42 |