Assay Detail
Binding
CHEMBL930493
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Activity at androgen receptor in human Saos2 cells assessed as IL6 repression
42
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SAOS-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.15 | 10.30 |
| Efficacy | 21 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 2 | 10.30 |
| CHEMBL427898 | — | — | 2 | 9.70 |
| CHEMBL256769 | — | — | 2 | 9.70 |
| CHEMBL257151 | — | — | 2 | 9.52 |
| CHEMBL258397 | — | — | 2 | 9.10 |
| CHEMBL253535 | — | — | 2 | 8.96 |
| CHEMBL427731 | — | — | 2 | 8.92 |
| CHEMBL401711 | — | — | 2 | 8.72 |
| CHEMBL256768 | — | — | 2 | 8.55 |
| CHEMBL256977 | — | — | 2 | 8.00 |
| CHEMBL256947 | — | — | 2 | 7.92 |
| CHEMBL401629 | — | — | 2 | 7.85 |
| CHEMBL450933 | — | — | 2 | 7.68 |
| CHEMBL257751 | — | — | 2 | 7.66 |
| CHEMBL450334 | — | — | 2 | 7.40 |
| CHEMBL258190 | — | — | 2 | 7.30 |
| CHEMBL403219 | — | — | 2 | 7.05 |
| CHEMBL258241 | — | — | 2 | 7.00 |
| CHEMBL253746 | — | — | 2 | 6.95 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 2 | 6.63 |
| CHEMBL402136 | — | — | 2 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL256769 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL427898 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL257151 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL258397 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL253535 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL427731 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL401711 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL256768 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL256977 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL256947 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL401629 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL450933 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL257751 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL450334 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL258190 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL403219 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL258241 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL253746 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL402136 | — | IC50 | = | 477.0 | nM | 6.32 |
| CHEMBL258241 | — | Efficacy | = | 50.0 | % | - |
| CHEMBL27769 | STANOLONE | Efficacy | = | 100.0 | % | - |
| CHEMBL409 | BICALUTAMIDE | Efficacy | = | 28.0 | % | - |
| CHEMBL402136 | — | Efficacy | = | 42.0 | % | - |
| CHEMBL450334 | — | Efficacy | = | 91.0 | % | - |
| CHEMBL257751 | — | Efficacy | = | 93.0 | % | - |
| CHEMBL403219 | — | Efficacy | = | 76.0 | % | - |
| CHEMBL253535 | — | Efficacy | = | 97.0 | % | - |
| CHEMBL401629 | — | Efficacy | = | 97.0 | % | - |
| CHEMBL253746 | — | Efficacy | = | 54.0 | % | - |
| CHEMBL427731 | — | Efficacy | = | 96.0 | % | - |
| CHEMBL257151 | — | Efficacy | = | 99.0 | % | - |
| CHEMBL256947 | — | Efficacy | = | 70.0 | % | - |
| CHEMBL427898 | — | Efficacy | = | 110.0 | % | - |
| CHEMBL256769 | — | Efficacy | = | 112.0 | % | - |
| CHEMBL450933 | — | Efficacy | = | 97.0 | % | - |
| CHEMBL256977 | — | Efficacy | = | 84.0 | % | - |
| CHEMBL258397 | — | Efficacy | = | 55.0 | % | - |
| CHEMBL256768 | — | Efficacy | = | 76.0 | % | - |
| CHEMBL401711 | — | Efficacy | = | 104.0 | % | - |
| CHEMBL258190 | — | Efficacy | = | 72.0 | % | - |