Assay Detail
Functional
CHEMBL899661
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.35 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.51 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.85 |
| CHEMBL235661 | — | — | 1 | 6.77 |
| CHEMBL393320 | — | — | 1 | 6.72 |
| CHEMBL238001 | — | — | 1 | 6.60 |
| CHEMBL237999 | — | — | 1 | 6.52 |
| CHEMBL235811 | — | — | 1 | 6.48 |
| CHEMBL235445 | — | — | 1 | 6.38 |
| CHEMBL235872 | — | — | 1 | 6.28 |
| CHEMBL428021 | — | — | 1 | 6.18 |
| CHEMBL235003 | — | — | 1 | 6.14 |
| CHEMBL238000 | — | — | 1 | 6.07 |
| CHEMBL393319 | — | — | 1 | 6.04 |
| CHEMBL235871 | — | — | 1 | 6.04 |
| CHEMBL391648 | — | — | 1 | 5.70 |
| CHEMBL237971 | — | — | 1 | 5.24 |
| CHEMBL236699 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL235661 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL393320 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL238001 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL237999 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL235811 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL235445 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL235872 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL428021 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL235003 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL238000 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL393319 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL235871 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL391648 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL237971 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL236699 | — | IC50 | > | 10000.0 | nM | - |