Assay Detail
Binding
CHEMBL5335599
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Induction of androgen receptor degradation in human LNCaP cells incubated for 24 hrs by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| 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 |
|---|---|---|---|
| EC50 | 12 | 5.52 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5400213 | — | — | 1 | 5.89 |
| CHEMBL5411468 | — | — | 1 | 5.86 |
| CHEMBL5420162 | — | — | 1 | 5.81 |
| CHEMBL5413706 | — | — | 1 | 5.78 |
| CHEMBL5409426 | — | — | 1 | 5.58 |
| CHEMBL5407635 | — | — | 1 | 5.55 |
| CHEMBL5404028 | — | — | 1 | 5.49 |
| CHEMBL5412123 | — | — | 1 | 5.48 |
| CHEMBL5414716 | — | — | 1 | 5.41 |
| CHEMBL5402908 | — | — | 1 | 5.32 |
| CHEMBL5425503 | — | — | 1 | 5.24 |
| CHEMBL2105738 | GALETERONE | 3.0 | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5400213 | — | EC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL5411468 | — | EC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL5420162 | — | EC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL5413706 | — | EC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL5409426 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5407635 | — | EC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL5404028 | — | EC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL5412123 | — | EC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL5414716 | — | EC50 | = | 3880.0 | nM | 5.41 |
| CHEMBL5402908 | — | EC50 | = | 4760.0 | nM | 5.32 |
| CHEMBL5425503 | — | EC50 | = | 5720.0 | nM | 5.24 |
| CHEMBL2105738 | GALETERONE | EC50 | = | 14400.0 | nM | 4.84 |