Assay Detail
Functional
CHEMBL833228
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity against mutant androgen receptor of LNCap cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| 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 | 5.34 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.40 |
| CHEMBL365921 | — | — | 1 | 5.73 |
| CHEMBL364393 | — | — | 1 | 5.62 |
| CHEMBL365650 | — | — | 1 | 5.59 |
| CHEMBL189600 | — | — | 1 | 5.58 |
| CHEMBL188857 | — | — | 1 | 5.46 |
| CHEMBL362566 | — | — | 1 | 5.41 |
| CHEMBL187605 | — | — | 1 | 5.36 |
| CHEMBL188129 | — | — | 1 | 5.35 |
| CHEMBL365482 | — | — | 1 | 5.32 |
| CHEMBL188803 | — | — | 1 | 5.30 |
| CHEMBL188545 | — | — | 1 | 5.23 |
| CHEMBL371392 | — | — | 1 | 5.17 |
| CHEMBL188261 | — | — | 1 | 4.98 |
| CHEMBL426623 | — | — | 1 | 4.52 |
| CHEMBL447184 | — | — | 1 | 4.47 |
| CHEMBL188297 | — | — | 1 | - |
| CHEMBL185880 | — | — | 1 | - |
| CHEMBL188681 | — | — | 1 | - |
| CHEMBL414845 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL365921 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL364393 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL365650 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL189600 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL188857 | — | IC50 | = | 3510.0 | nM | 5.46 |
| CHEMBL362566 | — | IC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL187605 | — | IC50 | = | 4380.0 | nM | 5.36 |
| CHEMBL188129 | — | IC50 | = | 4430.0 | nM | 5.35 |
| CHEMBL365482 | — | IC50 | = | 4750.0 | nM | 5.32 |
| CHEMBL188803 | — | IC50 | = | 4970.0 | nM | 5.30 |
| CHEMBL188545 | — | IC50 | = | 5860.0 | nM | 5.23 |
| CHEMBL371392 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL188261 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL426623 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL447184 | — | IC50 | = | 33700.0 | nM | 4.47 |
| CHEMBL188297 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL185880 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL188681 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL414845 | — | IC50 | > | 5000.0 | nM | - |