Assay Detail
Functional
CHEMBL5264674
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Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | VCaP |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.79 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740749 | — | — | 1 | 9.47 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 7.06 |
| CHEMBL1916251 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740749 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 87.4 | nM | 7.06 |
| CHEMBL1916251 | — | IC50 | = | 147.9 | nM | 6.83 |