Assay Detail
Binding
CHEMBL4717253
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Antagonist activity at human full-length MCR assessed as inhibition of receptor binding to co-activator peptide by PathHunter assay
30
Total Activities
30
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
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.38 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1393 | SPIRONOLACTONE | 4.0 | 1 | 7.96 |
| CHEMBL4792628 | — | — | 1 | 7.82 |
| CHEMBL4439903 | — | — | 1 | 7.68 |
| CHEMBL4759836 | — | — | 1 | 7.52 |
| CHEMBL4798697 | — | — | 1 | 7.48 |
| CHEMBL4764165 | — | — | 1 | 7.48 |
| CHEMBL4794194 | — | — | 1 | 7.22 |
| CHEMBL4777170 | — | — | 1 | 7.16 |
| CHEMBL4776613 | — | — | 1 | 7.01 |
| CHEMBL4563704 | — | — | 1 | 6.94 |
| CHEMBL4790021 | — | — | 1 | 6.70 |
| CHEMBL4746794 | — | — | 1 | 6.70 |
| CHEMBL1095097 | EPLERENONE | 4.0 | 1 | 6.61 |
| CHEMBL4755269 | — | — | 1 | 6.56 |
| CHEMBL4749536 | — | — | 1 | 6.48 |
| CHEMBL4742925 | — | — | 1 | 6.28 |
| CHEMBL4754975 | — | — | 1 | 6.03 |
| CHEMBL4796191 | — | — | 1 | 6.02 |
| CHEMBL4748904 | — | — | 1 | 5.77 |
| CHEMBL4792176 | — | — | 1 | 5.72 |
| CHEMBL4747722 | — | — | 1 | 5.72 |
| CHEMBL4760159 | — | — | 1 | 5.72 |
| CHEMBL4759690 | — | — | 1 | 5.67 |
| CHEMBL4756852 | — | — | 1 | 5.64 |
| CHEMBL4777887 | — | — | 1 | 5.57 |
| CHEMBL4746832 | — | — | 1 | 5.40 |
| CHEMBL4798873 | — | — | 1 | 5.32 |
| CHEMBL4763926 | — | — | 1 | 5.10 |
| CHEMBL4794041 | — | — | 1 | 5.01 |
| CHEMBL4780739 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1393 | SPIRONOLACTONE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4792628 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4439903 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4759836 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4798697 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4764165 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4794194 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4777170 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4776613 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4563704 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4790021 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4746794 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1095097 | EPLERENONE | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4755269 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4749536 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4742925 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4754975 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4796191 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4748904 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4792176 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4747722 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4760159 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4759690 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4756852 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL4777887 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4746832 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4798873 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4763926 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4794041 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4780739 | — | IC50 | = | 10000.0 | nM | 5.00 |