Assay Detail
Binding
CHEMBL828029
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory concentration against Cytochrome P450 17 expressed in Escherichia coli
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.09 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL74661 | — | — | 1 | 7.30 |
| CHEMBL75474 | — | — | 1 | 6.52 |
| CHEMBL77062 | — | — | 1 | 6.30 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 6.10 |
| CHEMBL77789 | — | — | 1 | 6.04 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 5.96 |
| CHEMBL78222 | — | — | 1 | 5.90 |
| CHEMBL74606 | — | — | 1 | 5.42 |
| CHEMBL363364 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL74661 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL75474 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL77062 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL77789 | — | IC50 | = | 915.0 | nM | 6.04 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL78222 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL74606 | — | IC50 | = | 3810.0 | nM | 5.42 |
| CHEMBL363364 | — | IC50 | = | 5817.4 | nM | 5.24 |