Assay Detail
Binding
CHEMBL2421744
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Inhibition of human CYP17 expressed in Escherichia coli using 1,2[3H]-progesterone as substrate in presence of NADPH
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 16 | 6.72 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2420683 | — | — | 1 | 7.96 |
| CHEMBL2420684 | — | — | 1 | 7.80 |
| CHEMBL2420674 | — | — | 1 | 7.19 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 7.14 |
| CHEMBL2420681 | — | — | 1 | 7.03 |
| CHEMBL2420675 | — | — | 1 | 6.97 |
| CHEMBL2420677 | — | — | 1 | 6.83 |
| CHEMBL2420682 | — | — | 1 | 6.73 |
| CHEMBL2420687 | — | — | 1 | 6.53 |
| CHEMBL2420678 | — | — | 1 | 6.43 |
| CHEMBL2420679 | — | — | 1 | 6.34 |
| CHEMBL2420680 | — | — | 1 | 6.28 |
| CHEMBL2420676 | — | — | 1 | 6.28 |
| CHEMBL2420685 | — | — | 1 | 6.20 |
| CHEMBL2420688 | — | — | 1 | 5.99 |
| CHEMBL2420686 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2420683 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2420684 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2420674 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2420681 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2420675 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL2420677 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL2420682 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL2420687 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL2420678 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL2420679 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL2420680 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL2420676 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL2420685 | — | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL2420688 | — | IC50 | = | 1028.0 | nM | 5.99 |
| CHEMBL2420686 | — | IC50 | = | 1520.0 | nM | 5.82 |