Assay Detail
Functional
CHEMBL1212405
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human wild type AR expressed in human MDA-MB-435 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 | MDA-MB-435 |
| 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 | 7.11 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1210783 | — | — | 1 | 8.13 |
| CHEMBL1210151 | — | — | 1 | 8.13 |
| CHEMBL1210033 | — | — | 1 | 8.03 |
| CHEMBL1210152 | — | — | 1 | 7.96 |
| CHEMBL1210842 | — | — | 1 | 7.92 |
| CHEMBL1209903 | — | — | 1 | 7.85 |
| CHEMBL1209972 | — | — | 1 | 7.80 |
| CHEMBL1210910 | — | — | 1 | 7.62 |
| CHEMBL1210214 | — | — | 1 | 7.51 |
| CHEMBL1210908 | — | — | 1 | 7.50 |
| CHEMBL1210150 | — | — | 1 | 7.43 |
| CHEMBL1210034 | — | — | 1 | 7.41 |
| CHEMBL1209970 | — | — | 1 | 7.27 |
| CHEMBL1208805 | — | — | 1 | 7.27 |
| CHEMBL1209973 | — | — | 1 | 7.19 |
| CHEMBL1209906 | — | — | 1 | 7.16 |
| CHEMBL1210036 | — | — | 1 | 7.07 |
| CHEMBL1210090 | — | — | 1 | 7.00 |
| CHEMBL1209904 | — | — | 1 | 6.89 |
| CHEMBL1208812 | — | — | 1 | 6.89 |
| CHEMBL1210091 | — | — | 1 | 6.77 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.76 |
| CHEMBL1210909 | — | — | 1 | 6.74 |
| CHEMBL1210035 | — | — | 1 | 6.69 |
| CHEMBL1209905 | — | — | 1 | 6.67 |
| CHEMBL1210907 | — | — | 1 | 6.50 |
| CHEMBL1209971 | — | — | 1 | 6.06 |
| CHEMBL1210841 | — | — | 1 | 6.06 |
| CHEMBL1210840 | — | — | 1 | 5.67 |
| CHEMBL1210843 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1210783 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1210151 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1210033 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL1210152 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1210842 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1209903 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1209972 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1210910 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1210214 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1210908 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1210150 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1210034 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1209970 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1208805 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1209973 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1209906 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1210036 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1210090 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL1209904 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1208812 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL1210091 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL1210909 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL1210035 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL1209905 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL1210907 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL1209971 | — | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL1210841 | — | IC50 | = | 873.0 | nM | 6.06 |
| CHEMBL1210840 | — | IC50 | = | 2144.0 | nM | 5.67 |
| CHEMBL1210843 | — | IC50 | = | 3900.0 | nM | 5.41 |