Assay Detail
Binding
CHEMBL1006441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CYP17 expressed in Escherichia coli coexpressed with cytochrome P450 reductase
39
Total Activities
39
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
Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.19 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 7.14 |
| CHEMBL505550 | — | — | 1 | 7.00 |
| CHEMBL501198 | — | — | 1 | 6.95 |
| CHEMBL454217 | — | — | 1 | 6.93 |
| CHEMBL501460 | — | — | 1 | 6.78 |
| CHEMBL499882 | — | — | 1 | 6.55 |
| CHEMBL498523 | — | — | 1 | 6.52 |
| CHEMBL496468 | — | — | 1 | 6.51 |
| CHEMBL527112 | — | — | 1 | 6.46 |
| CHEMBL500680 | — | — | 1 | 6.43 |
| CHEMBL502542 | — | — | 1 | 6.41 |
| CHEMBL497500 | — | — | 1 | 6.35 |
| CHEMBL498522 | — | — | 1 | 6.34 |
| CHEMBL449343 | — | — | 1 | 6.24 |
| CHEMBL500139 | — | — | 1 | 6.12 |
| CHEMBL526293 | — | — | 1 | 6.11 |
| CHEMBL277535 | BIFONAZOLE | 3.0 | 1 | 6.10 |
| CHEMBL497499 | — | — | 1 | 6.04 |
| CHEMBL526104 | — | — | 1 | 5.98 |
| CHEMBL445171 | — | — | 1 | 5.96 |
| CHEMBL501446 | — | — | 1 | 5.89 |
| CHEMBL443865 | — | — | 1 | 5.85 |
| CHEMBL500679 | — | — | 1 | 5.77 |
| CHEMBL496257 | — | — | 1 | 5.70 |
| CHEMBL497851 | — | — | 1 | 5.68 |
| CHEMBL500425 | — | — | 1 | 5.66 |
| CHEMBL498534 | — | — | 1 | 5.64 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 5.56 |
| CHEMBL498641 | — | — | 1 | 5.51 |
| CHEMBL502802 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254328 | ABIRATERONE | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL505550 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL501198 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL454217 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL501460 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL499882 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL498523 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL496468 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL527112 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL500680 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL502542 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL497500 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL498522 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL449343 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL500139 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL526293 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL277535 | BIFONAZOLE | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL497499 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL526104 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL445171 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL501446 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL443865 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL500679 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL496257 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL497851 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL500425 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL498534 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL498641 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL502802 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL524989 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL504098 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL526722 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL442568 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL498642 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL524681 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL500140 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL503503 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL496258 | — | IC50 | > | 5000.0 | nM | - |