Assay Detail
Binding
CHEMBL3399802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP11B2 in human V79MZ cells using [3H]-11-deoxycorticosterone as substrate incubated for 1 hr prior to substrate addition measured after 45 mins by HPLC analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | V79MZ |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.03 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | 4.0 | 1 | 9.70 |
| CHEMBL3397605 | — | — | 1 | 9.52 |
| CHEMBL3397600 | — | — | 1 | 9.30 |
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 9.10 |
| CHEMBL3397603 | — | — | 1 | 8.96 |
| CHEMBL3397607 | — | — | 1 | 8.66 |
| CHEMBL3397599 | — | — | 1 | 7.96 |
| CHEMBL509971 | — | — | 1 | 7.92 |
| CHEMBL3397604 | — | — | 1 | 7.62 |
| CHEMBL62811 | — | — | 1 | 7.55 |
| CHEMBL3397597 | — | — | 1 | 7.39 |
| CHEMBL3397602 | — | — | 1 | 7.05 |
| CHEMBL3397609 | — | — | 1 | 6.71 |
| CHEMBL3397606 | — | — | 1 | 6.64 |
| CHEMBL3397601 | — | — | 1 | 6.44 |
| CHEMBL3397598 | — | — | 1 | - |
| CHEMBL3397608 | — | — | 1 | - |
| CHEMBL3397610 | — | — | 1 | - |
| CHEMBL3397611 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3397605 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3397600 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL9298 | FADROZOLE | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3397603 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3397607 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3397599 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL509971 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3397604 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL62811 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3397597 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3397602 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3397609 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL3397606 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL3397601 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL3397598 | — | IC50 | - | — | - | |
| CHEMBL3397608 | — | IC50 | - | — | - | |
| CHEMBL3397610 | — | IC50 | - | — | - | |
| CHEMBL3397611 | — | IC50 | - | — | - |