Assay Detail
Binding
CHEMBL925709
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Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membrane
37
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Type-1 angiotensin II receptor A (CHEMBL329) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and biological evaluation of AT1 angiotensin II receptor antagonists based on the pyrazolo[3,4-b]pyridine and related heteroaromatic bicyclic systems.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.17 | 9.40 |
| Ki | 3 | 7.52 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7550 | L-158809 | — | 1 | 9.40 |
| CHEMBL408403 | ANGIOTENSIN II | 4.0 | 1 | 9.40 |
| CHEMBL315104 | — | — | 1 | 9.10 |
| CHEMBL1069 | VALSARTAN | 4.0 | 1 | 8.47 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 8.17 |
| CHEMBL86247 | — | — | 1 | 8.16 |
| CHEMBL358359 | — | — | 1 | 7.85 |
| CHEMBL259114 | — | — | 1 | 7.75 |
| CHEMBL315444 | — | — | 1 | 7.60 |
| CHEMBL259353 | — | — | 1 | 7.41 |
| CHEMBL258685 | — | — | 1 | 7.28 |
| CHEMBL408188 | — | — | 1 | 7.16 |
| CHEMBL262098 | — | — | 1 | 7.12 |
| CHEMBL146275 | — | — | 1 | 7.10 |
| CHEMBL410105 | — | — | 1 | 7.09 |
| CHEMBL265208 | — | — | 1 | 7.05 |
| CHEMBL410325 | — | — | 1 | 7.02 |
| CHEMBL409744 | — | — | 1 | 6.97 |
| CHEMBL260578 | — | — | 1 | 6.94 |
| CHEMBL265958 | — | — | 1 | 6.91 |
| CHEMBL261765 | — | — | 1 | 6.91 |
| CHEMBL258891 | — | — | 1 | 6.84 |
| CHEMBL261248 | — | — | 1 | 6.81 |
| CHEMBL408227 | — | — | 1 | 6.78 |
| CHEMBL409095 | — | — | 1 | 6.59 |
| CHEMBL409722 | — | — | 1 | 6.59 |
| CHEMBL265452 | — | — | 1 | 6.54 |
| CHEMBL259575 | — | — | 1 | 6.37 |
| CHEMBL410487 | — | — | 1 | 6.34 |
| CHEMBL427738 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7550 | L-158809 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL408403 | ANGIOTENSIN II | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL315104 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1069 | VALSARTAN | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL191 | LOSARTAN | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL86247 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL358359 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL259114 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL315444 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL259353 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL258685 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL408188 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL262098 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL146275 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL410105 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL265208 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL410325 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL409744 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL260578 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL261765 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL265958 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL258891 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL261248 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL408227 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL409095 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL409722 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL265452 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL259575 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL410487 | — | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL427738 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL410125 | — | IC50 | = | 598.0 | nM | 6.22 |
| CHEMBL265697 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL259116 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL258684 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL408187 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL264946 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL259397 | — | IC50 | > | 10000.0 | nM | - |