Assay Detail
Binding
CHEMBL839595
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Binding affinity for androgen receptor in human MDA-453 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.09 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL367375 | — | — | 1 | 8.52 |
| CHEMBL178333 | — | — | 1 | 8.30 |
| CHEMBL369542 | — | — | 1 | 8.05 |
| CHEMBL361445 | — | — | 1 | 7.72 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 7.37 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.19 |
| CHEMBL184981 | — | — | 1 | 7.08 |
| CHEMBL182412 | — | — | 1 | 7.00 |
| CHEMBL182593 | — | — | 1 | 6.80 |
| CHEMBL180681 | — | — | 1 | 6.77 |
| CHEMBL427502 | — | — | 1 | 6.37 |
| CHEMBL183882 | — | — | 1 | 5.55 |
| CHEMBL182993 | — | — | 1 | 5.50 |
| CHEMBL183173 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL367375 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL178333 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL369542 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL361445 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL184981 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL182412 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL182593 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL180681 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL427502 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL183882 | — | Ki | = | 2810.0 | nM | 5.55 |
| CHEMBL182993 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL183173 | — | Ki | > | 5000.0 | nM | - |