Assay Detail
Binding
CHEMBL877304
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Inhibition of mutant T877A Androgen receptor in human LNCaP cells
7
Total Activities
7
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 |
|---|---|---|---|
| IC50 | 7 | 7.08 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183882 | — | — | 1 | 7.64 |
| CHEMBL182993 | — | — | 1 | 7.52 |
| CHEMBL182593 | — | — | 1 | 7.39 |
| CHEMBL427502 | — | — | 1 | 7.23 |
| CHEMBL182412 | — | — | 1 | 7.18 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.40 |
| CHEMBL183173 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183882 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL182993 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL182593 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL427502 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL182412 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL183173 | — | IC50 | = | 631.0 | nM | 6.20 |