Assay Detail
Binding
CHEMBL4622650
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Antagonistic activity at AR in human 22Rv1 cells assessed as reduction in cell number by CCK8 assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CWR22R |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.49 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 6.64 |
| CHEMBL4648793 | — | — | 1 | 5.62 |
| CHEMBL4640248 | — | — | 1 | 5.48 |
| CHEMBL4634960 | — | — | 1 | 5.48 |
| CHEMBL4641012 | — | — | 1 | 5.44 |
| CHEMBL4642678 | — | — | 1 | 5.36 |
| CHEMBL2023820 | — | — | 1 | 5.33 |
| CHEMBL4646593 | — | — | 1 | 5.24 |
| CHEMBL4644092 | — | — | 1 | 5.19 |
| CHEMBL4642187 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4648793 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4640248 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4634960 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4641012 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4642678 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2023820 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4646593 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4644092 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4642187 | — | IC50 | = | 8100.0 | nM | 5.09 |