Assay Detail
Binding
CHEMBL5136137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mineralocorticoid receptor S810L mutant expressed in CHO-K1 cells assessed as inhibition of aldosterone-induced transcriptional activity incubated for 24 hrs in presence of 0.5 nM aldosterone by Steady-Glo reagent based reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 2 | 6.77 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 7.00 |
| CHEMBL2181929 | MT-3995 | 2.0 | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1095097 | EPLERENONE | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL2181929 | MT-3995 | IC50 | = | 288.0 | nM | 6.54 |