Assay Detail
Binding
CHEMBL3783933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CYP17A1 expressed in HEK293 cell microsomes using [3H]-pregnenolone as substrate incubated for 45 mins by scintillation proximity assay in presence of NADPH
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.21 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3782020 | — | — | 1 | 8.70 |
| CHEMBL3780658 | — | — | 1 | 8.52 |
| CHEMBL3780266 | — | — | 1 | 8.40 |
| CHEMBL3780743 | — | — | 1 | 8.40 |
| CHEMBL3781112 | — | — | 1 | 8.30 |
| CHEMBL3780226 | — | — | 1 | 8.30 |
| CHEMBL3780048 | — | — | 1 | 8.30 |
| CHEMBL2147034 | — | — | 1 | 8.22 |
| CHEMBL3781487 | — | — | 1 | 8.10 |
| CHEMBL3781910 | — | — | 1 | 8.10 |
| CHEMBL2147041 | — | — | 1 | 7.72 |
| CHEMBL2147035 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3782020 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3780658 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3780266 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3780743 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3781112 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3780226 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3780048 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2147034 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3781487 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3781910 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2147041 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2147035 | — | IC50 | = | 37.0 | nM | 7.43 |