Assay Detail
Binding
CHEMBL908918
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Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in rat hepatic membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Further studies on imidazo[4,5-b]pyridine AT1 angiotensin II receptor antagonists. Effects of the transformation of the 4-phenylquinoline backbone into 4-phenylisoquinolinone or 1-phenylindene scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.67 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87327 | — | — | 1 | 8.38 |
| CHEMBL216747 | — | — | 1 | 8.28 |
| CHEMBL441859 | — | — | 1 | 8.24 |
| CHEMBL217659 | — | — | 1 | 8.21 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 8.17 |
| CHEMBL86247 | — | — | 1 | 8.16 |
| CHEMBL314315 | — | — | 1 | 8.11 |
| CHEMBL84573 | — | — | 1 | 8.05 |
| CHEMBL384936 | — | — | 1 | 7.96 |
| CHEMBL384168 | — | — | 1 | 7.82 |
| CHEMBL387075 | — | — | 1 | 7.33 |
| CHEMBL425071 | — | — | 1 | 7.30 |
| CHEMBL386667 | — | — | 1 | 7.28 |
| CHEMBL214840 | — | — | 1 | 7.27 |
| CHEMBL385513 | — | — | 1 | 7.26 |
| CHEMBL217622 | — | — | 1 | 7.22 |
| CHEMBL266727 | — | — | 1 | 7.00 |
| CHEMBL437722 | — | — | 1 | 6.88 |
| CHEMBL217131 | — | — | 1 | 6.86 |
| CHEMBL217451 | — | — | 1 | - |
| CHEMBL214924 | — | — | 1 | - |
| CHEMBL384747 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87327 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL216747 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL441859 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL217659 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL191 | LOSARTAN | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL86247 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL314315 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL84573 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL384936 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL384168 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL387075 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL425071 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL386667 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL214840 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL385513 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL217622 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL266727 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL437722 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL217131 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL217451 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL214924 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL384747 | — | IC50 | > | 300.0 | nM | - |