Assay Detail
Functional
CHEMBL4325014
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Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
4
Total Activities
4
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 Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.53 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4528598 | — | — | 1 | 8.70 |
| CHEMBL4525203 | — | — | 1 | 8.22 |
| CHEMBL1916251 | — | — | 1 | 6.74 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4528598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4525203 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1916251 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL1082407 | ENZALUTAMIDE | IC50 | = | 364.0 | nM | 6.44 |