Assay Detail
Functional
CHEMBL935527
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Agonist activity at human androgen receptor in CV1 cells by transcriptional activation assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| 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 |
|---|---|---|---|
| EC50 | 21 | 8.04 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224263 | — | — | 1 | 8.96 |
| CHEMBL256326 | — | — | 1 | 8.89 |
| CHEMBL402039 | — | — | 1 | 8.70 |
| CHEMBL401805 | — | — | 1 | 8.70 |
| CHEMBL257396 | — | — | 1 | 8.49 |
| CHEMBL429311 | — | — | 1 | 8.42 |
| CHEMBL255655 | — | — | 1 | 8.38 |
| CHEMBL402835 | — | — | 1 | 8.28 |
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 8.24 |
| CHEMBL256330 | — | — | 1 | 8.23 |
| CHEMBL436644 | — | — | 1 | 8.18 |
| CHEMBL404512 | — | — | 1 | 7.96 |
| CHEMBL257379 | — | — | 1 | 7.72 |
| CHEMBL256284 | — | — | 1 | 7.64 |
| CHEMBL404483 | — | — | 1 | 7.64 |
| CHEMBL255918 | — | — | 1 | 7.55 |
| CHEMBL256126 | — | — | 1 | 7.52 |
| CHEMBL254798 | — | — | 1 | 7.46 |
| CHEMBL256544 | — | — | 1 | 7.44 |
| CHEMBL257988 | — | — | 1 | 7.38 |
| CHEMBL404568 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224263 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL256326 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL402039 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL401805 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL257396 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL429311 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL255655 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL402835 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL27769 | STANOLONE | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL256330 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL436644 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL404512 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL257379 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL256284 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL404483 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL255918 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL256126 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL254798 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL256544 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL257988 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL404568 | — | EC50 | = | 77.0 | nM | 7.11 |