Assay Detail
Binding
CHEMBL4124785
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CYP11B2 expressed in Chinese hamster V79 cell mitochondria assessed as reduction in aldosterone production using deoxycorticosterone as substrate after 1.5 hrs in presence of NADPH by HTRF assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | V79 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.94 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | 4.0 | 1 | 8.92 |
| CHEMBL4127675 | — | — | 1 | 8.66 |
| CHEMBL4126893 | — | — | 1 | 8.66 |
| CHEMBL4127904 | — | — | 1 | 8.64 |
| CHEMBL4125850 | — | — | 1 | 8.60 |
| CHEMBL4129296 | — | — | 1 | 8.49 |
| CHEMBL4128315 | — | — | 1 | 8.43 |
| CHEMBL4129177 | — | — | 1 | 8.40 |
| CHEMBL4125736 | — | — | 1 | 8.38 |
| CHEMBL4129619 | — | — | 1 | 8.33 |
| CHEMBL4128167 | — | — | 1 | 8.27 |
| CHEMBL4127082 | — | — | 1 | 8.17 |
| CHEMBL4129549 | — | — | 1 | 8.04 |
| CHEMBL4129146 | — | — | 1 | 7.92 |
| CHEMBL4126118 | — | — | 1 | 7.89 |
| CHEMBL4127939 | — | — | 1 | 7.85 |
| CHEMBL4125707 | — | — | 1 | 7.58 |
| CHEMBL4128736 | — | — | 1 | 7.54 |
| CHEMBL4126932 | — | — | 1 | 7.47 |
| CHEMBL4129577 | — | — | 1 | 7.15 |
| CHEMBL4126275 | — | — | 1 | 7.14 |
| CHEMBL4128486 | — | — | 1 | 6.82 |
| CHEMBL4128329 | — | — | 1 | 6.55 |
| CHEMBL4127095 | — | — | 1 | 6.54 |
| CHEMBL4128829 | — | — | 1 | - |
| CHEMBL4129567 | — | — | 1 | - |
| CHEMBL4129712 | — | — | 1 | - |
| CHEMBL4127248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4127675 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4126893 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4127904 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4125850 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4129296 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4128315 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4129177 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4125736 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4129619 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4128167 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4127082 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4129549 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4129146 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4126118 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4127939 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4125707 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4128736 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4126932 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4129577 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4126275 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4128486 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4128329 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4127095 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4128829 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4129567 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4129712 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4127248 | — | IC50 | > | 1000.0 | nM | - |