Assay Detail
Binding
CHEMBL3381815
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Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.71 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3337831 | — | — | 1 | 7.75 |
| CHEMBL3337825 | — | — | 1 | 7.48 |
| CHEMBL3337821 | — | — | 1 | 7.44 |
| CHEMBL1929039 | — | — | 1 | 7.37 |
| CHEMBL3337823 | — | — | 1 | 7.35 |
| CHEMBL3337824 | — | — | 1 | 7.31 |
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 7.22 |
| CHEMBL3337731 | — | — | 1 | 7.19 |
| CHEMBL3337829 | — | — | 1 | 7.15 |
| CHEMBL2419301 | — | — | 1 | 7.08 |
| CHEMBL3337734 | — | — | 1 | 6.89 |
| CHEMBL3337726 | — | — | 1 | 6.80 |
| CHEMBL3337725 | — | — | 1 | 6.77 |
| CHEMBL3337730 | — | — | 1 | 6.75 |
| CHEMBL3337832 | — | — | 1 | 6.75 |
| CHEMBL3337728 | — | — | 1 | 6.46 |
| CHEMBL3337822 | — | — | 1 | 6.37 |
| CHEMBL3337828 | — | — | 1 | 6.31 |
| CHEMBL3337830 | — | — | 1 | 6.27 |
| CHEMBL3337727 | — | — | 1 | 6.22 |
| CHEMBL3337733 | — | — | 1 | 6.17 |
| CHEMBL3337729 | — | — | 1 | 6.02 |
| CHEMBL3337735 | — | — | 1 | 6.00 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 5.89 |
| CHEMBL3337724 | — | — | 1 | 5.85 |
| CHEMBL3337827 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3337831 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3337825 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3337821 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1929039 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3337823 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3337824 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3337731 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3337829 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2419301 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3337734 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3337726 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3337725 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3337730 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3337832 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3337728 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3337822 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3337828 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3337830 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3337727 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3337733 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL3337729 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL3337735 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3337724 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3337827 | — | IC50 | = | 2000.0 | nM | 5.70 |