Assay Detail
Binding
CHEMBL869334
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Inhibition of rat AR-mediated reporter gene expression in COS7 cells
40
Total Activities
40
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.22 | 8.82 |
| Activity | 14 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166444 | METRIBOLONE | 2.0 | 1 | 8.82 |
| CHEMBL379527 | — | — | 1 | 7.54 |
| CHEMBL207706 | — | — | 1 | 7.52 |
| CHEMBL207106 | — | — | 1 | 7.28 |
| CHEMBL382892 | — | — | 1 | 6.96 |
| CHEMBL377653 | — | — | 1 | 6.96 |
| CHEMBL380133 | — | — | 1 | 6.89 |
| CHEMBL382640 | — | — | 1 | 6.43 |
| CHEMBL206909 | — | — | 1 | 6.24 |
| CHEMBL207168 | — | — | 1 | 6.20 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 6.07 |
| CHEMBL207510 | — | — | 1 | 6.06 |
| CHEMBL445661 | — | — | 1 | 6.04 |
| CHEMBL378087 | — | — | 1 | 6.03 |
| CHEMBL207518 | — | — | 1 | 6.00 |
| CHEMBL378733 | — | — | 1 | 5.82 |
| CHEMBL207509 | — | — | 1 | 5.68 |
| CHEMBL207550 | — | — | 1 | 5.64 |
| CHEMBL210634 | — | — | 1 | 5.55 |
| CHEMBL377611 | — | — | 1 | 5.55 |
| CHEMBL207339 | — | — | 1 | 5.52 |
| CHEMBL379244 | — | — | 1 | 5.47 |
| CHEMBL208088 | — | — | 1 | 5.43 |
| CHEMBL383485 | — | — | 1 | 5.42 |
| CHEMBL210924 | — | — | 1 | 5.35 |
| CHEMBL210570 | — | — | 1 | 5.30 |
| CHEMBL207629 | — | — | 1 | - |
| CHEMBL382767 | — | — | 1 | - |
| CHEMBL379031 | — | — | 1 | - |
| CHEMBL383703 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166444 | METRIBOLONE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL379527 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL207706 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL207106 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL382892 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL377653 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL380133 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL382640 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL206909 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL207168 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL207510 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL445661 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL378087 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL207518 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL378733 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL207509 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL207550 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL210634 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL377611 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL207339 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL379244 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL208088 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL383485 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL210924 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL210570 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL381801 | — | Activity | - | — | - | |
| CHEMBL438607 | — | Activity | - | — | - | |
| CHEMBL383039 | — | Activity | - | — | - | |
| CHEMBL381109 | — | Activity | - | — | - | |
| CHEMBL207656 | — | Activity | - | — | - | |
| CHEMBL377748 | — | Activity | - | — | - | |
| CHEMBL379084 | — | Activity | - | — | - | |
| CHEMBL210265 | — | Activity | - | — | - | |
| CHEMBL208087 | — | Activity | - | — | - | |
| CHEMBL206785 | — | Activity | - | — | - | |
| CHEMBL383703 | — | Activity | - | — | - | |
| CHEMBL379031 | — | Activity | - | — | - | |
| CHEMBL382767 | — | Activity | - | — | - | |
| CHEMBL207629 | — | Activity | - | — | - |