Assay Detail
Functional
CHEMBL1919237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human AR overexpressed in human LNCAP cells by luciferase reporter gene assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.09 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1916247 | — | — | 1 | 7.80 |
| CHEMBL1916245 | — | — | 1 | 7.70 |
| CHEMBL1916246 | — | — | 1 | 7.52 |
| CHEMBL1916237 | — | — | 1 | 7.50 |
| CHEMBL1916244 | — | — | 1 | 7.38 |
| CHEMBL1914477 | — | — | 1 | 7.27 |
| CHEMBL1916251 | — | — | 1 | 7.23 |
| CHEMBL1916238 | — | — | 1 | 7.16 |
| CHEMBL1916248 | — | — | 1 | 7.16 |
| CHEMBL1916243 | — | — | 1 | 7.12 |
| CHEMBL1916242 | — | — | 1 | 7.09 |
| CHEMBL1916252 | — | — | 1 | 7.05 |
| CHEMBL1916239 | — | — | 1 | 6.90 |
| CHEMBL1916249 | — | — | 1 | 6.87 |
| CHEMBL1916250 | — | — | 1 | 6.87 |
| CHEMBL1916412 | — | — | 1 | 6.84 |
| CHEMBL1916240 | — | — | 1 | 6.79 |
| CHEMBL1916253 | — | — | 1 | 6.79 |
| CHEMBL1916236 | — | — | 1 | 6.76 |
| CHEMBL1916254 | — | — | 1 | 6.76 |
| CHEMBL1916241 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1916247 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1916245 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1916246 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1916237 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1916244 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1914477 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1916251 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1916238 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1916248 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1916243 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1916242 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1916252 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1916239 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL1916249 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL1916250 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL1916412 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL1916240 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL1916253 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL1916236 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL1916254 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL1916241 | — | IC50 | = | 519.0 | nM | 6.29 |