Assay Detail
Binding
CHEMBL933063
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DHT from human androgen receptor in MDA453 cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 31 | 7.41 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403668 | — | — | 1 | 9.00 |
| CHEMBL272574 | — | — | 1 | 8.62 |
| CHEMBL446626 | — | — | 1 | 8.52 |
| CHEMBL402807 | — | — | 1 | 8.52 |
| CHEMBL257668 | — | — | 1 | 8.52 |
| CHEMBL272509 | — | — | 1 | 8.52 |
| CHEMBL403213 | — | — | 1 | 8.40 |
| CHEMBL255331 | — | — | 1 | 8.14 |
| CHEMBL403061 | — | — | 1 | 7.92 |
| CHEMBL403039 | — | — | 1 | 7.77 |
| CHEMBL271262 | — | — | 1 | 7.77 |
| CHEMBL403214 | — | — | 1 | 7.77 |
| CHEMBL403669 | — | — | 1 | 7.77 |
| CHEMBL255216 | — | — | 1 | 7.75 |
| CHEMBL255776 | — | — | 1 | 7.68 |
| CHEMBL271261 | — | — | 1 | 7.57 |
| CHEMBL404315 | — | — | 1 | 7.40 |
| CHEMBL272510 | — | — | 1 | 7.39 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.37 |
| CHEMBL402930 | — | — | 1 | 7.28 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.19 |
| CHEMBL255367 | — | — | 1 | 7.11 |
| CHEMBL270586 | — | — | 1 | 6.66 |
| CHEMBL367364 | — | — | 1 | 6.44 |
| CHEMBL270450 | — | — | 1 | 6.42 |
| CHEMBL404506 | — | — | 1 | 6.39 |
| CHEMBL437214 | — | — | 1 | 6.31 |
| CHEMBL271924 | — | — | 1 | 6.16 |
| CHEMBL271925 | — | — | 1 | 5.96 |
| CHEMBL427721 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403668 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL272574 | — | Ki | = | 2.41 | nM | 8.62 |
| CHEMBL446626 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL402807 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL257668 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL272509 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL403213 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL255331 | — | Ki | = | 7.18 | nM | 8.14 |
| CHEMBL403061 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL403039 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL271262 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL403214 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL403669 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL255216 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL255776 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL271261 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL404315 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL272510 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL402930 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL255367 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL270586 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL367364 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL270450 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL404506 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL437214 | — | Ki | = | 486.0 | nM | 6.31 |
| CHEMBL271924 | — | Ki | = | 692.0 | nM | 6.16 |
| CHEMBL271925 | — | Ki | = | 1110.0 | nM | 5.96 |
| CHEMBL427721 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL255157 | — | Ki | = | 4100.0 | nM | 5.39 |