Assay Detail
Binding
CHEMBL933554
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Displacement of [3H]DHT from human Androgen receptor in human MDA-MB-453 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.90 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224263 | — | — | 1 | 9.05 |
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 9.05 |
| CHEMBL257379 | — | — | 1 | 8.96 |
| CHEMBL402835 | — | — | 1 | 8.89 |
| CHEMBL404483 | — | — | 1 | 8.62 |
| CHEMBL429311 | — | — | 1 | 8.59 |
| CHEMBL401805 | — | — | 1 | 8.23 |
| CHEMBL256326 | — | — | 1 | 8.18 |
| CHEMBL256330 | — | — | 1 | 8.08 |
| CHEMBL402039 | — | — | 1 | 8.03 |
| CHEMBL404512 | — | — | 1 | 7.82 |
| CHEMBL256126 | — | — | 1 | 7.75 |
| CHEMBL256284 | — | — | 1 | 7.75 |
| CHEMBL436644 | — | — | 1 | 7.66 |
| CHEMBL254798 | — | — | 1 | 7.50 |
| CHEMBL404568 | — | — | 1 | 6.96 |
| CHEMBL404222 | — | — | 1 | 6.82 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.82 |
| CHEMBL257387 | — | — | 1 | 6.75 |
| CHEMBL257988 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224263 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL27769 | STANOLONE | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL257379 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL402835 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL404483 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL429311 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL401805 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL256326 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL256330 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL402039 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL404512 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL256126 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL256284 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL436644 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL254798 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL404568 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL404222 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL257387 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL257988 | — | Ki | = | 281.0 | nM | 6.55 |