Assay Detail
Binding
CHEMBL1929757
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Displacement of [3H]dexomethasone from GR
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 | 21 | 5.74 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929041 | — | — | 1 | 6.70 |
| CHEMBL1929042 | — | — | 1 | 6.33 |
| CHEMBL1928878 | — | — | 1 | 6.02 |
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 5.85 |
| CHEMBL1929040 | — | — | 1 | 5.77 |
| CHEMBL1929039 | — | — | 1 | 5.75 |
| CHEMBL1929036 | — | — | 1 | 5.60 |
| CHEMBL1928877 | — | — | 1 | 5.46 |
| CHEMBL1928874 | — | — | 1 | 5.26 |
| CHEMBL1928872 | — | — | 1 | 5.25 |
| CHEMBL1928882 | — | — | 1 | 5.16 |
| CHEMBL1928879 | — | — | 1 | - |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | - |
| CHEMBL1928881 | — | — | 1 | - |
| CHEMBL1928880 | — | — | 1 | - |
| CHEMBL1928869 | — | — | 1 | - |
| CHEMBL1928876 | — | — | 1 | - |
| CHEMBL1928875 | — | — | 1 | - |
| CHEMBL1928873 | — | — | 1 | - |
| CHEMBL1928871 | — | — | 1 | - |
| CHEMBL1928870 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929041 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1929042 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1928878 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1929040 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1929039 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1929036 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1928877 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1928874 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL1928872 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1928882 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL1928879 | — | IC50 | - | — | - | |
| CHEMBL1095097 | EPLERENONE | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928881 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928880 | — | IC50 | - | — | - | |
| CHEMBL1928869 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928876 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928875 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1928873 | — | IC50 | - | — | - | |
| CHEMBL1928871 | — | IC50 | - | — | - | |
| CHEMBL1928870 | — | IC50 | - | — | - |