Assay Detail
Functional
CHEMBL1121349
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Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
19
Total Activities
19
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
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.11 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1099086 | — | — | 1 | 7.92 |
| CHEMBL1095862 | — | — | 1 | 7.75 |
| CHEMBL1095863 | — | — | 1 | 7.52 |
| CHEMBL1098173 | — | — | 1 | 7.29 |
| CHEMBL1099142 | — | — | 1 | 7.26 |
| CHEMBL1097855 | — | — | 1 | 7.10 |
| CHEMBL1095224 | — | — | 1 | 7.05 |
| CHEMBL1098171 | — | — | 1 | 6.96 |
| CHEMBL1095223 | — | — | 1 | 6.70 |
| CHEMBL1099141 | — | — | 1 | 6.40 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.26 |
| CHEMBL1094117 | — | — | 1 | - |
| CHEMBL1099087 | — | — | 1 | - |
| CHEMBL1098174 | — | — | 1 | - |
| CHEMBL1098172 | — | — | 1 | - |
| CHEMBL1095864 | — | — | 1 | - |
| CHEMBL1095861 | — | — | 1 | - |
| CHEMBL1099158 | — | — | 1 | - |
| CHEMBL1099140 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1099086 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1095862 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1095863 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1098173 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1099142 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1097855 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1095224 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1098171 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1095223 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1099141 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1094117 | — | IC50 | - | — | - | |
| CHEMBL1099087 | — | IC50 | - | — | - | |
| CHEMBL1098174 | — | IC50 | - | — | - | |
| CHEMBL1098172 | — | IC50 | - | — | - | |
| CHEMBL1095864 | — | IC50 | - | — | - | |
| CHEMBL1095861 | — | IC50 | - | — | - | |
| CHEMBL1099158 | — | IC50 | - | — | - | |
| CHEMBL1099140 | — | IC50 | - | — | - |