Assay Detail
Binding
CHEMBL2339068
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Androgen receptor T877A mutant (unknown origin) expressed in Freestyle293F cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 17 | 7.05 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 8.59 |
| CHEMBL2337509 | — | — | 1 | 8.09 |
| CHEMBL2337512 | — | — | 1 | 7.80 |
| CHEMBL2337511 | — | — | 1 | 7.75 |
| CHEMBL2337506 | — | — | 1 | 7.52 |
| CHEMBL2337508 | — | — | 1 | 7.44 |
| CHEMBL2337510 | — | — | 1 | 7.38 |
| CHEMBL2337505 | — | — | 1 | 7.23 |
| CHEMBL2337516 | — | — | 1 | 7.06 |
| CHEMBL2337515 | — | — | 1 | 7.01 |
| CHEMBL2337513 | — | — | 1 | 7.00 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.92 |
| CHEMBL2337507 | — | — | 1 | 6.89 |
| CHEMBL2337517 | — | — | 1 | 6.62 |
| CHEMBL2337519 | — | — | 1 | 5.77 |
| CHEMBL2337514 | — | — | 1 | 5.52 |
| CHEMBL2337518 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2337509 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL2337512 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2337511 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2337506 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2337508 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2337510 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2337505 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2337516 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL2337515 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL2337513 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2337507 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2337517 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2337519 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2337514 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2337518 | — | IC50 | = | 5300.0 | nM | 5.28 |