Assay Detail
Binding
CHEMBL1212404
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Displacement of [3H]DHT from AR in human MDA-MB-453 cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-453 |
| 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 |
|---|---|---|---|
| Ki | 30 | 7.58 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1210152 | — | — | 1 | 8.46 |
| CHEMBL1210910 | — | — | 1 | 8.43 |
| CHEMBL1209973 | — | — | 1 | 8.24 |
| CHEMBL1210214 | — | — | 1 | 8.21 |
| CHEMBL1210033 | — | — | 1 | 8.18 |
| CHEMBL1210783 | — | — | 1 | 8.05 |
| CHEMBL1210151 | — | — | 1 | 8.03 |
| CHEMBL1210842 | — | — | 1 | 7.96 |
| CHEMBL1210090 | — | — | 1 | 7.92 |
| CHEMBL1210908 | — | — | 1 | 7.85 |
| CHEMBL1209903 | — | — | 1 | 7.85 |
| CHEMBL1210036 | — | — | 1 | 7.80 |
| CHEMBL1210840 | — | — | 1 | 7.70 |
| CHEMBL1208812 | — | — | 1 | 7.68 |
| CHEMBL1210150 | — | — | 1 | 7.66 |
| CHEMBL1209970 | — | — | 1 | 7.64 |
| CHEMBL1210034 | — | — | 1 | 7.54 |
| CHEMBL1208805 | — | — | 1 | 7.50 |
| CHEMBL1209906 | — | — | 1 | 7.44 |
| CHEMBL1210909 | — | — | 1 | 7.43 |
| CHEMBL1209905 | — | — | 1 | 7.41 |
| CHEMBL1209972 | — | — | 1 | 7.40 |
| CHEMBL1210841 | — | — | 1 | 7.30 |
| CHEMBL1210035 | — | — | 1 | 7.25 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.19 |
| CHEMBL1209904 | — | — | 1 | 7.08 |
| CHEMBL1210091 | — | — | 1 | 7.03 |
| CHEMBL1209971 | — | — | 1 | 7.01 |
| CHEMBL1210907 | — | — | 1 | 6.75 |
| CHEMBL1210843 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1210152 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1210910 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1209973 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL1210214 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL1210033 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL1210783 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1210151 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL1210842 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1210090 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1210908 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1209903 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1210036 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1210840 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1208812 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1210150 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1209970 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1210034 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1208805 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL1209906 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL1210909 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1209905 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1209972 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL1210841 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1210035 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1209904 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL1210091 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL1209971 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL1210907 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL1210843 | — | Ki | = | 3600.0 | nM | 5.44 |