Assay Detail
Binding
CHEMBL2339064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at Androgen receptor T877A mutant in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP-hr |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 6.05 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 7.82 |
| CHEMBL2337509 | — | — | 1 | 7.70 |
| CHEMBL2337506 | — | — | 1 | 6.19 |
| CHEMBL2337505 | — | — | 1 | 5.32 |
| CHEMBL2337512 | — | — | 1 | 5.29 |
| CHEMBL2337511 | — | — | 1 | 5.00 |
| CHEMBL2337510 | — | — | 1 | 5.00 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | - |
| CHEMBL2337515 | — | — | 1 | - |
| CHEMBL2337514 | — | — | 1 | - |
| CHEMBL2337513 | — | — | 1 | - |
| CHEMBL2337508 | — | — | 1 | - |
| CHEMBL2337507 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2337509 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2337506 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2337505 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2337512 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2337511 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2337510 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL409 | BICALUTAMIDE | EC50 | > | 10000.0 | nM | - |
| CHEMBL2337515 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2337514 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2337513 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2337508 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2337507 | — | EC50 | > | 10000.0 | nM | - |