Assay Detail
Binding
CHEMBL825228
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Binding affinity for mutant T877A Androgen receptor in human LNCaP cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| 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 | 13 | 8.22 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180681 | — | — | 1 | 11.00 |
| CHEMBL361445 | — | — | 1 | 9.30 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 8.70 |
| CHEMBL178333 | — | — | 1 | 8.70 |
| CHEMBL182593 | — | — | 1 | 8.22 |
| CHEMBL369542 | — | — | 1 | 8.05 |
| CHEMBL182993 | — | — | 1 | 8.05 |
| CHEMBL182412 | — | — | 1 | 7.72 |
| CHEMBL183882 | — | — | 1 | 7.70 |
| CHEMBL184981 | — | — | 1 | 7.55 |
| CHEMBL427502 | — | — | 1 | 7.48 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.46 |
| CHEMBL183173 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180681 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL361445 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL178333 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL182593 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL369542 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL182993 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL182412 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL183882 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL184981 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL427502 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL183173 | — | Ki | = | 115.0 | nM | 6.94 |