Assay Detail
Binding
CHEMBL887363
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Binding affinity to human androgen receptor expressed in CV1 cells
41
Total Activities
41
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 7.15 | 9.70 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 9.70 |
| CHEMBL436784 | — | — | 1 | 8.82 |
| CHEMBL3706898 | — | — | 1 | 8.05 |
| CHEMBL3706874 | — | — | 1 | 7.96 |
| CHEMBL3706899 | — | — | 1 | 7.89 |
| CHEMBL3706888 | — | — | 1 | 7.82 |
| CHEMBL3706907 | — | — | 1 | 7.80 |
| CHEMBL3706897 | — | — | 1 | 7.70 |
| CHEMBL3706878 | — | — | 1 | 7.54 |
| CHEMBL3706894 | — | — | 1 | 7.52 |
| CHEMBL3706896 | — | — | 1 | 7.52 |
| CHEMBL3706889 | — | — | 1 | 7.44 |
| CHEMBL3706875 | — | — | 1 | 7.43 |
| CHEMBL3706879 | — | — | 1 | 7.30 |
| CHEMBL3706911 | — | — | 1 | 7.25 |
| CHEMBL3706910 | — | — | 1 | 7.23 |
| CHEMBL3706881 | — | — | 1 | 7.19 |
| CHEMBL350877 | — | — | 1 | 7.14 |
| CHEMBL3706909 | — | — | 1 | 7.13 |
| CHEMBL3706908 | — | — | 1 | 7.11 |
| CHEMBL3706880 | — | — | 1 | 7.10 |
| CHEMBL3706877 | — | — | 1 | 7.08 |
| CHEMBL3706883 | — | — | 1 | 6.96 |
| CHEMBL3706884 | — | — | 1 | 6.93 |
| CHEMBL3706882 | — | — | 1 | 6.87 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.82 |
| CHEMBL3706903 | — | — | 1 | 6.80 |
| CHEMBL3706885 | — | — | 1 | 6.79 |
| CHEMBL3706891 | — | — | 1 | 6.79 |
| CHEMBL3706895 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL436784 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3706898 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3706874 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3706899 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3706888 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3706907 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3706897 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3706878 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3706894 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3706896 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3706889 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3706875 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL3706879 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3706911 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3706910 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL3706881 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL350877 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL3706909 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL3706908 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL3706880 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL3706877 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL3706883 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL3706884 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL3706882 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL409 | BICALUTAMIDE | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL3706903 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL3706885 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL3706891 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL3706895 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL3706876 | — | Ki | = | 407.0 | nM | 6.39 |
| CHEMBL3706893 | — | Ki | = | 463.0 | nM | 6.33 |
| CHEMBL3706900 | — | Ki | = | 641.0 | nM | 6.19 |
| CHEMBL3706901 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL3706892 | — | Ki | = | 761.0 | nM | 6.12 |
| CHEMBL3706902 | — | Ki | = | 869.0 | nM | 6.06 |
| CHEMBL3706886 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3706887 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3706904 | — | Activity | - | — | - | |
| CHEMBL3706905 | — | Activity | - | — | - | |
| CHEMBL3706906 | — | Activity | - | — | - |