Assay Detail
Binding
CHEMBL881287
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Inhibitory concentration against human cytochrome P450 11B1 expressed in fission yeast, incubated with [14C]deoxycorticosterone
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.86 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 8.00 |
| CHEMBL194472 | — | — | 1 | 7.09 |
| CHEMBL370822 | — | — | 1 | 6.68 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 6.65 |
| CHEMBL196796 | — | — | 1 | 6.16 |
| CHEMBL193653 | — | — | 1 | 6.09 |
| CHEMBL195629 | — | — | 1 | 6.07 |
| CHEMBL195996 | — | — | 1 | 5.88 |
| CHEMBL362968 | — | — | 1 | 5.80 |
| CHEMBL197576 | — | — | 1 | 5.60 |
| CHEMBL371430 | — | — | 1 | 5.57 |
| CHEMBL195571 | — | — | 1 | 5.57 |
| CHEMBL193534 | — | — | 1 | 5.53 |
| CHEMBL196328 | — | — | 1 | 5.35 |
| CHEMBL381014 | — | — | 1 | 5.31 |
| CHEMBL193343 | — | — | 1 | 5.27 |
| CHEMBL365735 | — | — | 1 | 5.24 |
| CHEMBL193556 | — | — | 1 | 5.20 |
| CHEMBL194277 | — | — | 1 | 5.12 |
| CHEMBL438802 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9298 | FADROZOLE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL194472 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL370822 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL196796 | — | IC50 | = | 691.0 | nM | 6.16 |
| CHEMBL193653 | — | IC50 | = | 805.0 | nM | 6.09 |
| CHEMBL195629 | — | IC50 | = | 849.0 | nM | 6.07 |
| CHEMBL195996 | — | IC50 | = | 1317.0 | nM | 5.88 |
| CHEMBL362968 | — | IC50 | = | 1577.0 | nM | 5.80 |
| CHEMBL197576 | — | IC50 | = | 2517.0 | nM | 5.60 |
| CHEMBL371430 | — | IC50 | = | 2724.0 | nM | 5.57 |
| CHEMBL195571 | — | IC50 | = | 2671.0 | nM | 5.57 |
| CHEMBL193534 | — | IC50 | = | 2939.0 | nM | 5.53 |
| CHEMBL196328 | — | IC50 | = | 4481.0 | nM | 5.35 |
| CHEMBL381014 | — | IC50 | = | 4898.0 | nM | 5.31 |
| CHEMBL193343 | — | IC50 | = | 5419.0 | nM | 5.27 |
| CHEMBL365735 | — | IC50 | = | 5826.0 | nM | 5.24 |
| CHEMBL193556 | — | IC50 | = | 6338.0 | nM | 5.20 |
| CHEMBL194277 | — | IC50 | = | 7553.0 | nM | 5.12 |
| CHEMBL438802 | — | IC50 | = | 10505.0 | nM | 4.98 |