Assay Detail
Functional
CHEMBL1212407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay
30
Total Activities
30
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
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.38 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1209903 | — | — | 1 | 7.60 |
| CHEMBL1210033 | — | — | 1 | 7.27 |
| CHEMBL1210842 | — | — | 1 | 7.16 |
| CHEMBL1210152 | — | — | 1 | 6.98 |
| CHEMBL1210034 | — | — | 1 | 6.98 |
| CHEMBL1209972 | — | — | 1 | 6.91 |
| CHEMBL1210783 | — | — | 1 | 6.90 |
| CHEMBL1210908 | — | — | 1 | 6.90 |
| CHEMBL1210151 | — | — | 1 | 6.82 |
| CHEMBL1210910 | — | — | 1 | 6.75 |
| CHEMBL1209970 | — | — | 1 | 6.75 |
| CHEMBL1210150 | — | — | 1 | 6.47 |
| CHEMBL1210214 | — | — | 1 | 6.42 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.40 |
| CHEMBL1209906 | — | — | 1 | 6.39 |
| CHEMBL1209904 | — | — | 1 | 6.26 |
| CHEMBL1209973 | — | — | 1 | 6.23 |
| CHEMBL1210036 | — | — | 1 | 6.22 |
| CHEMBL1208805 | — | — | 1 | 6.16 |
| CHEMBL1210090 | — | — | 1 | 6.01 |
| CHEMBL1210091 | — | — | 1 | 5.91 |
| CHEMBL1210909 | — | — | 1 | 5.89 |
| CHEMBL1210907 | — | — | 1 | 5.84 |
| CHEMBL1209905 | — | — | 1 | 5.79 |
| CHEMBL1210841 | — | — | 1 | 5.48 |
| CHEMBL1210035 | — | — | 1 | 5.46 |
| CHEMBL1209971 | — | — | 1 | 5.34 |
| CHEMBL1210843 | — | — | 1 | 5.30 |
| CHEMBL1210840 | — | — | 1 | - |
| CHEMBL1208812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1209903 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1210033 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1210842 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1210152 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL1210034 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL1209972 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL1210783 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL1210908 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL1210151 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1210910 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL1209970 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL1210150 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL1210214 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1209906 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL1209904 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL1209973 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1210036 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1208805 | — | IC50 | = | 685.0 | nM | 6.16 |
| CHEMBL1210090 | — | IC50 | = | 979.0 | nM | 6.01 |
| CHEMBL1210091 | — | IC50 | = | 1241.0 | nM | 5.91 |
| CHEMBL1210909 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL1210907 | — | IC50 | = | 1456.0 | nM | 5.84 |
| CHEMBL1209905 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL1210841 | — | IC50 | = | 3329.0 | nM | 5.48 |
| CHEMBL1210035 | — | IC50 | = | 3511.0 | nM | 5.46 |
| CHEMBL1209971 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1210843 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1210840 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1208812 | — | IC50 | > | 5000.0 | nM | - |