Assay Detail
Functional
CHEMBL933064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human androgen receptor in MDA453 cells by alkaline phosphatase reporter gene assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.93 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403668 | — | — | 1 | 8.15 |
| CHEMBL403669 | — | — | 1 | 8.15 |
| CHEMBL255331 | — | — | 1 | 8.00 |
| CHEMBL403214 | — | — | 1 | 7.96 |
| CHEMBL446626 | — | — | 1 | 7.80 |
| CHEMBL257668 | — | — | 1 | 7.80 |
| CHEMBL272574 | — | — | 1 | 7.72 |
| CHEMBL272509 | — | — | 1 | 7.72 |
| CHEMBL403061 | — | — | 1 | 7.70 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.58 |
| CHEMBL272510 | — | — | 1 | 7.44 |
| CHEMBL403213 | — | — | 1 | 7.42 |
| CHEMBL403039 | — | — | 1 | 7.40 |
| CHEMBL271261 | — | — | 1 | 7.16 |
| CHEMBL255216 | — | — | 1 | 7.06 |
| CHEMBL271262 | — | — | 1 | 6.92 |
| CHEMBL255776 | — | — | 1 | 6.89 |
| CHEMBL367364 | — | — | 1 | 6.82 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.76 |
| CHEMBL270586 | — | — | 1 | 6.46 |
| CHEMBL404506 | — | — | 1 | 6.46 |
| CHEMBL270450 | — | — | 1 | 6.32 |
| CHEMBL255367 | — | — | 1 | 6.30 |
| CHEMBL402930 | — | — | 1 | 6.17 |
| CHEMBL404315 | — | — | 1 | 6.11 |
| CHEMBL271924 | — | — | 1 | 5.94 |
| CHEMBL437214 | — | — | 1 | 5.64 |
| CHEMBL427721 | — | — | 1 | 5.54 |
| CHEMBL271925 | — | — | 1 | 5.48 |
| CHEMBL255157 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403668 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL403669 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL255331 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL403214 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL446626 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL257668 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL272574 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL272509 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL403061 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL491 | HYDROXYFLUTAMIDE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL272510 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL403213 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL403039 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL271261 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL255216 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL271262 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL255776 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL367364 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL270586 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL404506 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL270450 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL255367 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL402930 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL404315 | — | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL271924 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL437214 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL427721 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL271925 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL255157 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL402807 | — | IC50 | > | 5000.0 | nM | - |