Assay Detail
Functional
CHEMBL4411622
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Cytotoxicity against human 22Rv1 cells expressing full length androgen receptor H875Y point mutant assessed as reduction in cell viability after 48 hrs by MTS assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CWR22R |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Down-Regulation of the Androgen Receptor by G-Quadruplex Ligands Sensitizes Castration-Resistant Prostate Cancer Cells to Enzalutamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.09 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4468209 | — | — | 1 | 8.00 |
| CHEMBL4565909 | — | — | 1 | 7.00 |
| CHEMBL4526946 | — | — | 1 | 6.01 |
| CHEMBL4452581 | — | — | 1 | 5.61 |
| CHEMBL4453055 | — | — | 1 | 5.46 |
| CHEMBL4558509 | — | — | 1 | 5.43 |
| CHEMBL4519317 | — | — | 1 | 5.12 |
| CHEMBL4436828 | — | — | 1 | - |
| CHEMBL4566017 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4468209 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4565909 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4526946 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4452581 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL4453055 | — | IC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL4558509 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL4519317 | — | IC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL4436828 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4566017 | — | IC50 | > | 10000.0 | nM | - |