Assay Detail
ADMET
CHEMBL5335601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human CYP17A1 using progesterone as substrate incubated for 5 mins in presence of NADPH by LC-MS/MS analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.20 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 8.70 |
| CHEMBL2105738 | GALETERONE | 3.0 | 1 | 7.80 |
| CHEMBL5400213 | — | — | 1 | 7.00 |
| CHEMBL5413706 | — | — | 1 | 6.90 |
| CHEMBL5407635 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254328 | ABIRATERONE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2105738 | GALETERONE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5400213 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5413706 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5407635 | — | IC50 | = | 2590.0 | nM | 5.59 |