Assay Detail
Binding
CHEMBL4025651
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human CYP17 expressed in human A549 cell membranes using 17-alpha hydroxyprogesterone as substrate and NADPH as cofactor pretreated for 5 mins followed by substrate and cofactor addition after 60 mins by LC/MS analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| 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 novel 1,2,3,4-tetrahydrobenzo[4, 5]thieno[2, 3-c]pyridine derivatives as potent and selective CYP17 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.52 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4059780 | — | — | 1 | 7.70 |
| CHEMBL4064141 | — | — | 1 | 7.62 |
| CHEMBL4068802 | — | — | 1 | 7.61 |
| CHEMBL4101612 | — | — | 1 | 7.54 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 7.45 |
| CHEMBL4063960 | — | — | 1 | 7.35 |
| CHEMBL4091726 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4059780 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL4064141 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL4068802 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL4101612 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 35.8 | nM | 7.45 |
| CHEMBL4063960 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4091726 | — | IC50 | = | 45.4 | nM | 7.34 |