Assay Detail
Binding
CHEMBL911185
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Displacement of [3H]DHT from human androgen receptor expressed in MDA-MB-453 cells by whole cell receptor binding assay
13
Total Activities
13
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 | Expert |
Publication
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.89 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 9.70 |
| CHEMBL436784 | — | — | 1 | 8.82 |
| CHEMBL277378 | — | — | 1 | 8.36 |
| CHEMBL217324 | — | — | 1 | 8.20 |
| CHEMBL267260 | — | — | 1 | 8.15 |
| CHEMBL217769 | — | — | 1 | 8.15 |
| CHEMBL217402 | — | — | 1 | 8.13 |
| CHEMBL405835 | — | — | 1 | 7.27 |
| CHEMBL217428 | — | — | 1 | 7.24 |
| CHEMBL442240 | — | — | 1 | 7.19 |
| CHEMBL217168 | — | — | 1 | 6.82 |
| CHEMBL216949 | — | — | 1 | 6.65 |
| CHEMBL385509 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL436784 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL277378 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL217324 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL267260 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL217769 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL217402 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL405835 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL217428 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL442240 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL217168 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL216949 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL385509 | — | Ki | > | 10000.0 | nM | - |