Assay Detail
ADMET
CHEMBL4256958
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Inhibition of human membrane bound C-terminal His4-tagged CYP21A2 delta19H mutant assessed as reduction in progesterone hydroxylation measured after 10 mins in presence of NADPH/NADPH-cytochrome p450 reductase by GC/MS method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Inhibitors of cyp17a1
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.84 | 6.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105738 | GALETERONE | 3.0 | 1 | 6.61 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 6.53 |
| CHEMBL4209941 | — | — | 1 | 6.27 |
| CHEMBL4209916 | — | — | 1 | 6.08 |
| CHEMBL1921976 | ORTERONEL | 3.0 | 1 | 5.31 |
| CHEMBL4210141 | — | — | 1 | 5.06 |
| CHEMBL4280255 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105738 | GALETERONE | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL4209941 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL4209916 | — | IC50 | = | 831.0 | nM | 6.08 |
| CHEMBL1921976 | ORTERONEL | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL4210141 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4280255 | — | IC50 | = | 10300.0 | nM | 4.99 |