Assay Detail
Binding
CHEMBL1219277
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Inhibition of human CYP17 expressed in Escherichia coli
30
Total Activities
30
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
Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.25 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172779 | — | — | 1 | 7.28 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 7.14 |
| CHEMBL1172882 | — | — | 1 | 7.01 |
| CHEMBL1173260 | — | — | 1 | 6.73 |
| CHEMBL1171987 | — | — | 1 | 6.65 |
| CHEMBL1215664 | — | — | 1 | 6.61 |
| CHEMBL1173327 | — | — | 1 | 6.47 |
| CHEMBL1215732 | — | — | 1 | 6.41 |
| CHEMBL1215665 | — | — | 1 | 6.39 |
| CHEMBL1214739 | — | — | 1 | 6.36 |
| CHEMBL1214735 | — | — | 1 | 6.24 |
| CHEMBL1214660 | — | — | 1 | 6.22 |
| CHEMBL1214736 | — | — | 1 | 6.19 |
| CHEMBL1214737 | — | — | 1 | 6.12 |
| CHEMBL1215730 | — | — | 1 | 6.06 |
| CHEMBL1214662 | — | — | 1 | 5.86 |
| CHEMBL1215596 | — | — | 1 | 5.79 |
| CHEMBL1215731 | — | — | 1 | 5.75 |
| CHEMBL1214738 | — | — | 1 | 5.70 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 5.56 |
| CHEMBL1214661 | — | — | 1 | 5.48 |
| CHEMBL1215663 | — | — | 1 | 5.39 |
| CHEMBL1215729 | — | — | 1 | - |
| CHEMBL1214734 | — | — | 1 | - |
| CHEMBL1214664 | — | — | 1 | - |
| CHEMBL1214663 | — | — | 1 | - |
| CHEMBL551254 | — | — | 1 | - |
| CHEMBL934 | METYRAPONE | 4.0 | 1 | - |
| CHEMBL1215662 | — | — | 1 | - |
| CHEMBL1215595 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172779 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1172882 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1173260 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL1171987 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL1215664 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL1173327 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL1215732 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL1215665 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL1214739 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL1214735 | — | IC50 | = | 577.0 | nM | 6.24 |
| CHEMBL1214660 | — | IC50 | = | 598.0 | nM | 6.22 |
| CHEMBL1214736 | — | IC50 | = | 647.0 | nM | 6.19 |
| CHEMBL1214737 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL1215730 | — | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL1214662 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL1215596 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL1215731 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL1214738 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL1214661 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL1215663 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL1215729 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1214734 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1214664 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1214663 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL551254 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL934 | METYRAPONE | IC50 | > | 10000.0 | nM | - |
| CHEMBL1215662 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1215595 | — | IC50 | > | 5000.0 | nM | - |