Assay Detail
Binding
CHEMBL1929756
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 34 | 6.39 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929041 | — | — | 1 | 7.92 |
| CHEMBL1929042 | — | — | 1 | 7.68 |
| CHEMBL1928877 | — | — | 1 | 7.44 |
| CHEMBL1929039 | — | — | 1 | 7.39 |
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 7.31 |
| CHEMBL1928878 | — | — | 1 | 7.16 |
| CHEMBL1929040 | — | — | 1 | 7.12 |
| CHEMBL1929036 | — | — | 1 | 7.10 |
| CHEMBL1928884 | — | — | 1 | 6.58 |
| CHEMBL1928876 | — | — | 1 | 6.57 |
| CHEMBL1928875 | — | — | 1 | 6.51 |
| CHEMBL1929035 | — | — | 1 | 6.50 |
| CHEMBL1929034 | — | — | 1 | 6.37 |
| CHEMBL1929032 | — | — | 1 | 6.36 |
| CHEMBL1928872 | — | — | 1 | 6.29 |
| CHEMBL1928885 | — | — | 1 | 6.24 |
| CHEMBL1929037 | — | — | 1 | 6.23 |
| CHEMBL1928874 | — | — | 1 | 6.22 |
| CHEMBL1929038 | — | — | 1 | 6.16 |
| CHEMBL1929029 | — | — | 1 | 6.04 |
| CHEMBL1928883 | — | — | 1 | 6.02 |
| CHEMBL1929033 | — | — | 1 | 5.96 |
| CHEMBL1928882 | — | — | 1 | 5.96 |
| CHEMBL1928871 | — | — | 1 | 5.89 |
| CHEMBL1928869 | — | — | 1 | 5.70 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 5.58 |
| CHEMBL1929031 | — | — | 1 | 5.57 |
| CHEMBL1928870 | — | — | 1 | 5.39 |
| CHEMBL1928881 | — | — | 1 | 5.28 |
| CHEMBL1929030 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929041 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1929042 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1928877 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1929039 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1928878 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1929040 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1929036 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1928884 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1928876 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1928875 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1929035 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1929034 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1929032 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1928872 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1928885 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL1929037 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1928874 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1929038 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1929029 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1928883 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL1929033 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1928882 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1928871 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1928869 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1929031 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1928870 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL1928881 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL1929030 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL1929028 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928880 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928879 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928873 | — | IC50 | > | 10000.0 | nM | - |