Assay Detail
Functional
CHEMBL836730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity against androgen receptor of MDA-453 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.28 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188297 | — | — | 1 | 8.00 |
| CHEMBL365482 | — | — | 1 | 7.22 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.77 |
| CHEMBL362566 | — | — | 1 | 6.70 |
| CHEMBL364393 | — | — | 1 | 6.60 |
| CHEMBL189600 | — | — | 1 | 6.52 |
| CHEMBL426623 | — | — | 1 | 6.47 |
| CHEMBL371392 | — | — | 1 | 6.24 |
| CHEMBL365921 | — | — | 1 | 6.24 |
| CHEMBL414845 | — | — | 1 | 6.19 |
| CHEMBL188261 | — | — | 1 | 6.11 |
| CHEMBL187605 | — | — | 1 | 6.11 |
| CHEMBL185880 | — | — | 1 | 5.89 |
| CHEMBL188545 | — | — | 1 | 5.88 |
| CHEMBL188803 | — | — | 1 | 5.59 |
| CHEMBL188129 | — | — | 1 | 5.48 |
| CHEMBL447184 | — | — | 1 | 4.75 |
| CHEMBL188857 | — | — | 1 | - |
| CHEMBL188681 | — | — | 1 | - |
| CHEMBL365650 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188297 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL365482 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL362566 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL364393 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL189600 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL426623 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL371392 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL365921 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL414845 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL188261 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL187605 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL185880 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL188545 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL188803 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL188129 | — | IC50 | = | 3320.0 | nM | 5.48 |
| CHEMBL447184 | — | IC50 | = | 17900.0 | nM | 4.75 |
| CHEMBL188857 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL188681 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL365650 | — | IC50 | > | 5000.0 | nM | - |