Assay Detail
Binding
CHEMBL2339067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| 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 | 6.90 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337511 | — | — | 1 | 8.07 |
| CHEMBL2337516 | — | — | 1 | 7.96 |
| CHEMBL2337509 | — | — | 1 | 7.77 |
| CHEMBL2337510 | — | — | 1 | 7.77 |
| CHEMBL2337513 | — | — | 1 | 7.60 |
| CHEMBL2337517 | — | — | 1 | 7.21 |
| CHEMBL2337508 | — | — | 1 | 7.17 |
| CHEMBL2337506 | — | — | 1 | 7.09 |
| CHEMBL2337512 | — | — | 1 | 6.92 |
| CHEMBL2337519 | — | — | 1 | 6.54 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.48 |
| CHEMBL2337507 | — | — | 1 | 6.42 |
| CHEMBL2337518 | — | — | 1 | 6.40 |
| CHEMBL2337505 | — | — | 1 | 6.00 |
| CHEMBL2337514 | — | — | 1 | 5.77 |
| CHEMBL2337515 | — | — | 1 | 5.19 |
| CHEMBL27769 | STANOLONE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337511 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2337516 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2337509 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2337510 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2337513 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2337517 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2337508 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2337506 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2337512 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2337519 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2337507 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2337518 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2337505 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2337514 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2337515 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL27769 | STANOLONE | IC50 | > | 10000.0 | nM | - |