Assay Detail
Binding
CHEMBL2421741
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Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | V79MZh |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.12 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 8.20 |
| CHEMBL2420678 | — | — | 1 | 6.65 |
| CHEMBL2420674 | — | — | 1 | 6.63 |
| CHEMBL2420688 | — | — | 1 | 6.62 |
| CHEMBL2420682 | — | — | 1 | 6.61 |
| CHEMBL2420687 | — | — | 1 | 6.44 |
| CHEMBL2420681 | — | — | 1 | 6.35 |
| CHEMBL2420680 | — | — | 1 | 6.35 |
| CHEMBL2420676 | — | — | 1 | 5.94 |
| CHEMBL2420679 | — | — | 1 | 5.85 |
| CHEMBL2420675 | — | — | 1 | 5.79 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 5.79 |
| CHEMBL2420686 | — | — | 1 | 5.62 |
| CHEMBL2420684 | — | — | 1 | 5.55 |
| CHEMBL2420677 | — | — | 1 | 5.53 |
| CHEMBL2420683 | — | — | 1 | 5.15 |
| CHEMBL2420685 | — | — | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9298 | FADROZOLE | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2420678 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL2420674 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL2420688 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL2420682 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL2420687 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL2420681 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL2420680 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2420676 | — | IC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL2420679 | — | IC50 | = | 1415.0 | nM | 5.85 |
| CHEMBL2420675 | — | IC50 | = | 1609.0 | nM | 5.79 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL2420686 | — | IC50 | = | 2426.0 | nM | 5.62 |
| CHEMBL2420684 | — | IC50 | = | 2824.0 | nM | 5.55 |
| CHEMBL2420677 | — | IC50 | = | 2935.0 | nM | 5.53 |
| CHEMBL2420683 | — | IC50 | = | 7099.0 | nM | 5.15 |
| CHEMBL2420685 | — | IC50 | = | 12286.0 | nM | 4.91 |