Assay Detail
Binding
CHEMBL3592212
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at androgen receptor (unknown origin)
21
Total Activities
21
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 novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.03 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589383 | — | — | 1 | 7.92 |
| CHEMBL3589385 | — | — | 1 | 7.85 |
| CHEMBL3589381 | — | — | 1 | 7.74 |
| CHEMBL1082407 | ENZALUTAMIDE | 4.0 | 1 | 7.55 |
| CHEMBL3589380 | — | — | 1 | 7.47 |
| CHEMBL3183409 | APALUTAMIDE | 4.0 | 1 | 7.46 |
| CHEMBL3588961 | — | — | 1 | 7.39 |
| CHEMBL3588960 | — | — | 1 | 7.17 |
| CHEMBL3589387 | — | — | 1 | 6.90 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.79 |
| CHEMBL3589382 | — | — | 1 | 6.67 |
| CHEMBL3588964 | — | — | 1 | 6.63 |
| CHEMBL3588963 | — | — | 1 | 6.29 |
| CHEMBL3588968 | — | — | 1 | 6.24 |
| CHEMBL3588967 | — | — | 1 | 6.23 |
| CHEMBL3588962 | — | — | 1 | 6.10 |
| CHEMBL3589384 | — | — | 1 | - |
| CHEMBL3589386 | — | — | 1 | - |
| CHEMBL3589388 | — | — | 1 | - |
| CHEMBL3588969 | — | — | 1 | - |
| CHEMBL3588966 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589383 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL3589385 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL3589381 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL1082407 | ENZALUTAMIDE | Ki | = | 28.2 | nM | 7.55 |
| CHEMBL3589380 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL3183409 | APALUTAMIDE | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL3588961 | — | Ki | = | 40.6 | nM | 7.39 |
| CHEMBL3588960 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL3589387 | — | Ki | = | 126.1 | nM | 6.90 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 160.2 | nM | 6.79 |
| CHEMBL3589382 | — | Ki | = | 215.4 | nM | 6.67 |
| CHEMBL3588964 | — | Ki | = | 235.9 | nM | 6.63 |
| CHEMBL3588963 | — | Ki | = | 514.5 | nM | 6.29 |
| CHEMBL3588968 | — | Ki | = | 575.6 | nM | 6.24 |
| CHEMBL3588967 | — | Ki | = | 584.6 | nM | 6.23 |
| CHEMBL3588962 | — | Ki | = | 797.6 | nM | 6.10 |
| CHEMBL3589384 | — | Ki | - | — | - | |
| CHEMBL3589386 | — | Ki | - | — | - | |
| CHEMBL3589388 | — | Ki | - | — | - | |
| CHEMBL3588969 | — | Ki | - | — | - | |
| CHEMBL3588966 | — | Ki | - | — | - |