Assay Detail
Binding
CHEMBL5136136
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human wild-type mineralocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of aldosterone-induced transcriptional activity incubated for 24 hrs in presence of 1 nM aldosterone by Steady-Glo reagent based reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.13 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 8.06 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 6.75 |
| CHEMBL2181929 | MT-3995 | 2.0 | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL2181929 | MT-3995 | IC50 | = | 256.0 | nM | 6.59 |