Assay Detail
Functional
CHEMBL933552
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Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay
12
Total Activities
12
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 |
|---|---|---|---|
| IC50 | 12 | 7.07 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL404568 | — | — | 1 | 7.77 |
| CHEMBL255918 | — | — | 1 | 7.60 |
| CHEMBL257988 | — | — | 1 | 7.47 |
| CHEMBL256329 | — | — | 1 | 7.36 |
| CHEMBL256082 | — | — | 1 | 7.29 |
| CHEMBL404512 | — | — | 1 | 7.22 |
| CHEMBL224263 | — | — | 1 | 7.16 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.79 |
| CHEMBL436644 | — | — | 1 | 6.78 |
| CHEMBL254798 | — | — | 1 | 6.70 |
| CHEMBL404222 | — | — | 1 | 6.47 |
| CHEMBL257387 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL404568 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL255918 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL257988 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL256329 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL256082 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL404512 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL224263 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL436644 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL254798 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL404222 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL257387 | — | IC50 | = | 574.0 | nM | 6.24 |