Assay Detail
Binding
CHEMBL3265996
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mineralocorticoid receptor (unknown origin) by Gal4-based cellular assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.91 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3263768 | — | — | 1 | 8.66 |
| CHEMBL3263760 | — | — | 1 | 8.57 |
| CHEMBL3263766 | — | — | 1 | 8.55 |
| CHEMBL3263764 | — | — | 1 | 8.48 |
| CHEMBL3263762 | — | — | 1 | 8.43 |
| CHEMBL3263767 | — | — | 1 | 8.39 |
| CHEMBL3263763 | — | — | 1 | 8.37 |
| CHEMBL3263757 | — | — | 1 | 8.36 |
| CHEMBL3263752 | — | — | 1 | 8.35 |
| CHEMBL3263754 | — | — | 1 | 8.12 |
| CHEMBL3263750 | — | — | 1 | 8.05 |
| CHEMBL1215331 | PF-03882845 | 1.0 | 1 | 8.04 |
| CHEMBL3263765 | — | — | 1 | 8.03 |
| CHEMBL3263751 | — | — | 1 | 7.97 |
| CHEMBL1215130 | — | — | 1 | 7.82 |
| CHEMBL3263755 | — | — | 1 | 7.75 |
| CHEMBL3263761 | — | — | 1 | 7.75 |
| CHEMBL3263756 | — | — | 1 | 7.67 |
| CHEMBL1215197 | — | — | 1 | 7.59 |
| CHEMBL3263759 | — | — | 1 | 7.51 |
| CHEMBL3263758 | — | — | 1 | 7.25 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 6.91 |
| CHEMBL3263753 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3263768 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3263760 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3263766 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3263764 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3263762 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3263767 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3263763 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3263757 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3263752 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3263754 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3263750 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1215331 | PF-03882845 | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3263765 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3263751 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL1215130 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL3263755 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3263761 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL3263756 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL1215197 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL3263759 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL3263758 | — | IC50 | = | 55.9 | nM | 7.25 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3263753 | — | IC50 | = | 4450.0 | nM | 5.35 |