Assay Detail
Functional
CHEMBL1929764
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.05 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929042 | — | — | 1 | 7.82 |
| CHEMBL1929039 | — | — | 1 | 7.37 |
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 7.22 |
| CHEMBL1929041 | — | — | 1 | 7.16 |
| CHEMBL1929040 | — | — | 1 | 7.07 |
| CHEMBL1929036 | — | — | 1 | 6.82 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929042 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1929039 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1929041 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1929040 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1929036 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 1300.0 | nM | 5.89 |