Assay Detail
Binding
CHEMBL3418338
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Inhibition of human CYP11B2 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 | 7.24 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | 4.0 | 1 | 9.70 |
| CHEMBL9298 | FADROZOLE | 2.0 | 1 | 9.10 |
| CHEMBL3415172 | — | — | 1 | 8.66 |
| CHEMBL3313969 | — | — | 1 | 8.38 |
| CHEMBL3415171 | — | — | 1 | 8.15 |
| CHEMBL3415173 | — | — | 1 | 7.71 |
| CHEMBL3415166 | — | — | 1 | 7.69 |
| CHEMBL3415167 | — | — | 1 | 7.55 |
| CHEMBL3415175 | — | — | 1 | 7.37 |
| CHEMBL3415169 | — | — | 1 | 7.24 |
| CHEMBL3415155 | — | — | 1 | 7.20 |
| CHEMBL3415168 | — | — | 1 | 7.06 |
| CHEMBL2331699 | — | — | 1 | 7.05 |
| CHEMBL3415154 | — | — | 1 | 6.88 |
| CHEMBL3415153 | — | — | 1 | 6.76 |
| CHEMBL3415152 | — | — | 1 | 6.61 |
| CHEMBL3415174 | — | — | 1 | 6.47 |
| CHEMBL3415157 | — | — | 1 | 6.27 |
| CHEMBL3415163 | — | — | 1 | 6.15 |
| CHEMBL3415156 | — | — | 1 | 6.01 |
| CHEMBL3415170 | — | — | 1 | 5.93 |
| CHEMBL3415162 | — | — | 1 | 5.36 |
| CHEMBL3415161 | — | — | 1 | - |
| CHEMBL3415160 | — | — | 1 | - |
| CHEMBL3415159 | — | — | 1 | - |
| CHEMBL3415158 | — | — | 1 | - |
| CHEMBL3415164 | — | — | 1 | - |
| CHEMBL3415165 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL9298 | FADROZOLE | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3415172 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3313969 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3415171 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3415173 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL3415166 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL3415167 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL3415175 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL3415169 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL3415155 | — | IC50 | = | 62.5 | nM | 7.20 |
| CHEMBL3415168 | — | IC50 | = | 87.6 | nM | 7.06 |
| CHEMBL2331699 | — | IC50 | = | 89.7 | nM | 7.05 |
| CHEMBL3415154 | — | IC50 | = | 131.4 | nM | 6.88 |
| CHEMBL3415153 | — | IC50 | = | 172.2 | nM | 6.76 |
| CHEMBL3415152 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL3415174 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL3415157 | — | IC50 | = | 541.7 | nM | 6.27 |
| CHEMBL3415163 | — | IC50 | = | 707.7 | nM | 6.15 |
| CHEMBL3415156 | — | IC50 | = | 979.3 | nM | 6.01 |
| CHEMBL3415170 | — | IC50 | = | 1177.9 | nM | 5.93 |
| CHEMBL3415162 | — | IC50 | = | 4354.4 | nM | 5.36 |
| CHEMBL3415161 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415160 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415159 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415158 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415164 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3415165 | — | IC50 | > | 10000.0 | nM | - |