Assay Detail
Binding
CHEMBL4008023
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Antagonist activity at Gal4-fused human MR LBD (734 to 985 residues) expressed in CHO-K1 cells after 5 to 6 hrs by luciferase reporter gene assay
12
Total Activities
12
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
Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.43 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4104632 | — | — | 1 | 8.15 |
| CHEMBL2181927 | FINERENONE | 4.0 | 1 | 7.75 |
| CHEMBL4094464 | — | — | 1 | 7.75 |
| CHEMBL4066981 | — | — | 1 | 7.72 |
| CHEMBL4099077 | — | — | 1 | 7.64 |
| CHEMBL4096901 | — | — | 1 | 7.58 |
| CHEMBL2181926 | — | — | 1 | 7.55 |
| CHEMBL4102462 | — | — | 1 | 7.41 |
| CHEMBL4068008 | — | — | 1 | 7.33 |
| CHEMBL4089197 | — | — | 1 | 7.00 |
| CHEMBL4084504 | — | — | 1 | 6.80 |
| CHEMBL4081044 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4104632 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2181927 | FINERENONE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4094464 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4066981 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4099077 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4096901 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2181926 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4102462 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4068008 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4089197 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4084504 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4081044 | — | IC50 | = | 310.0 | nM | 6.51 |