Assay Detail
Binding
CHEMBL5335606
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at androgen receptor W741L mutant expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of androgen receptor incubated for 24 hrs by Steady-Glo assay
4
Total Activities
4
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 |
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 | 4 | 6.28 | 6.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5400213 | — | — | 1 | 6.43 |
| CHEMBL5413706 | — | — | 1 | 6.38 |
| CHEMBL5407635 | — | — | 1 | 6.31 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5400213 | — | IC50 | = | 371.3 | nM | 6.43 |
| CHEMBL5413706 | — | IC50 | = | 413.1 | nM | 6.38 |
| CHEMBL5407635 | — | IC50 | = | 490.2 | nM | 6.31 |
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 1031.0 | nM | 5.99 |