Assay Detail
Binding
CHEMBL3418339
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Inhibition of human CYP11B1 expressed in V79 MZh cells using [14C]-deoxycorticosterone substrate incubated for 6 hrs by HPTLC method
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | V79MZh |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.77 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | 4.0 | 1 | 8.54 |
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 8.20 |
| CHEMBL3415172 | — | — | 1 | 6.96 |
| CHEMBL3415171 | — | — | 1 | 6.37 |
| CHEMBL3313969 | — | — | 1 | 5.75 |
| CHEMBL3415166 | — | — | 1 | 5.74 |
| CHEMBL3415169 | — | — | 1 | 5.45 |
| CHEMBL3415167 | — | — | 1 | 5.41 |
| CHEMBL3415173 | — | — | 1 | 5.34 |
| CHEMBL3415175 | — | — | 1 | 5.24 |
| CHEMBL3415168 | — | — | 1 | 5.16 |
| CHEMBL3415152 | — | — | 1 | 5.10 |
| CHEMBL3415154 | — | — | 1 | 4.90 |
| CHEMBL3415153 | — | — | 1 | 4.79 |
| CHEMBL3415155 | — | — | 1 | 4.77 |
| CHEMBL2331699 | — | — | 1 | 4.53 |
| CHEMBL3415162 | — | — | 1 | - |
| CHEMBL3415157 | — | — | 1 | - |
| CHEMBL3415161 | — | — | 1 | - |
| CHEMBL3415174 | — | — | 1 | - |
| CHEMBL3415160 | — | — | 1 | - |
| CHEMBL3415159 | — | — | 1 | - |
| CHEMBL3415158 | — | — | 1 | - |
| CHEMBL3415170 | — | — | 1 | - |
| CHEMBL3415163 | — | — | 1 | - |
| CHEMBL3415165 | — | — | 1 | - |
| CHEMBL3415164 | — | — | 1 | - |
| CHEMBL3415156 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL9298 | FADROZOLE | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3415172 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3415171 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL3313969 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL3415166 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL3415169 | — | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL3415167 | — | IC50 | = | 3910.0 | nM | 5.41 |
| CHEMBL3415173 | — | IC50 | = | 4520.0 | nM | 5.34 |
| CHEMBL3415175 | — | IC50 | = | 5705.0 | nM | 5.24 |
| CHEMBL3415168 | — | IC50 | = | 6970.0 | nM | 5.16 |
| CHEMBL3415152 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3415154 | — | IC50 | = | 12620.0 | nM | 4.90 |
| CHEMBL3415153 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL3415155 | — | IC50 | = | 16990.0 | nM | 4.77 |
| CHEMBL2331699 | — | IC50 | = | 29540.0 | nM | 4.53 |
| CHEMBL3415162 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415157 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415161 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415174 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415160 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415159 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415158 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415163 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415165 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415164 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415156 | — | IC50 | > | 10000.0 | nM | - |