Assay Detail
Binding
CHEMBL5136122
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-aldosterone from recombinant human mineralocorticoid receptor expressed in baculovirus infected insect cells incubated overnight by liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Ki | 13 | 6.31 | 6.83 |
| IC50 | 3 | 7.08 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 8.02 |
| CHEMBL5181002 | — | — | 1 | 6.83 |
| CHEMBL5187656 | — | — | 1 | 6.82 |
| CHEMBL5174401 | — | — | 1 | 6.80 |
| CHEMBL5181278 | — | — | 1 | 6.79 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 6.65 |
| CHEMBL2181929 | MT-3995 | 2.0 | 1 | 6.56 |
| CHEMBL5171957 | — | — | 1 | 6.47 |
| CHEMBL5172350 | — | — | 1 | 6.22 |
| CHEMBL5184647 | — | — | 1 | 6.21 |
| CHEMBL5201004 | — | — | 1 | 6.13 |
| CHEMBL5176336 | — | — | 1 | 6.13 |
| CHEMBL5183454 | — | — | 1 | 6.09 |
| CHEMBL5207249 | — | — | 1 | 5.90 |
| CHEMBL5182687 | — | — | 1 | 5.86 |
| CHEMBL5186524 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 9.62 | nM | 8.02 |
| CHEMBL5181002 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL5187656 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL5174401 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL5181278 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL2181929 | MT-3995 | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL5171957 | — | Ki | = | 342.0 | nM | 6.47 |
| CHEMBL5172350 | — | Ki | = | 607.0 | nM | 6.22 |
| CHEMBL5184647 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL5201004 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL5176336 | — | Ki | = | 735.0 | nM | 6.13 |
| CHEMBL5183454 | — | Ki | = | 808.0 | nM | 6.09 |
| CHEMBL5207249 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL5182687 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL5186524 | — | Ki | = | 1920.0 | nM | 5.72 |