Assay Detail
Binding
CHEMBL5136126
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-dexamethasone from rat glucocorticoid receptor incubated overnight by liquid scintillation counting analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 22 | 4.43 | 4.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5197264 | — | — | 1 | 4.71 |
| CHEMBL5207249 | — | — | 1 | 4.65 |
| CHEMBL5207123 | — | — | 1 | 4.59 |
| CHEMBL5191961 | — | — | 1 | 4.54 |
| CHEMBL5181002 | — | — | 1 | 4.54 |
| CHEMBL5186524 | — | — | 1 | 4.42 |
| CHEMBL5201004 | — | — | 1 | 4.40 |
| CHEMBL5184647 | — | — | 1 | 4.38 |
| CHEMBL5181278 | — | — | 1 | 4.37 |
| CHEMBL5172350 | — | — | 1 | 4.35 |
| CHEMBL5176336 | — | — | 1 | 4.33 |
| CHEMBL5171957 | — | — | 1 | 4.26 |
| CHEMBL2181929 | MT-3995 | 2.0 | 1 | 4.08 |
| CHEMBL5182687 | — | — | 1 | - |
| CHEMBL5186231 | — | — | 1 | - |
| CHEMBL5173089 | — | — | 1 | - |
| CHEMBL5208644 | — | — | 1 | - |
| CHEMBL5182675 | — | — | 1 | - |
| CHEMBL5204612 | — | — | 1 | - |
| CHEMBL5174401 | — | — | 1 | - |
| CHEMBL5183454 | — | — | 1 | - |
| CHEMBL5187656 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5197264 | — | Ki | = | 19600.0 | nM | 4.71 |
| CHEMBL5207249 | — | Ki | = | 22200.0 | nM | 4.65 |
| CHEMBL5207123 | — | Ki | = | 25400.0 | nM | 4.59 |
| CHEMBL5191961 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL5181002 | — | Ki | = | 29100.0 | nM | 4.54 |
| CHEMBL5186524 | — | Ki | = | 37900.0 | nM | 4.42 |
| CHEMBL5201004 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL5184647 | — | Ki | = | 41500.0 | nM | 4.38 |
| CHEMBL5181278 | — | Ki | = | 43200.0 | nM | 4.37 |
| CHEMBL5172350 | — | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL5176336 | — | Ki | = | 47200.0 | nM | 4.33 |
| CHEMBL5171957 | — | Ki | = | 55200.0 | nM | 4.26 |
| CHEMBL2181929 | MT-3995 | Ki | = | 84200.0 | nM | 4.08 |
| CHEMBL5182687 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5186231 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5173089 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5208644 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5182675 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5204612 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5174401 | — | Ki | = | 136000.0 | nM | - |
| CHEMBL5183454 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5187656 | — | Ki | > | 100000.0 | nM | - |