Assay Detail
Binding
CHEMBL649306
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Displacement of [3H]angiotensin II from Angiotensin II type 1 receptor in rat adrenal cortical membrane
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.46 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL342553 | — | — | 1 | 9.24 |
| CHEMBL255111 | — | — | 1 | 8.90 |
| CHEMBL429847 | MILFASARTAN | 2.0 | 1 | 8.85 |
| CHEMBL344093 | — | — | 1 | 8.68 |
| CHEMBL144016 | — | — | 1 | 8.52 |
| CHEMBL358121 | — | — | 1 | 8.52 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 8.17 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.96 |
| CHEMBL144856 | — | — | 1 | 7.85 |
| CHEMBL144764 | — | — | 1 | 7.80 |
| CHEMBL142979 | — | — | 1 | 7.75 |
| CHEMBL144646 | — | — | 1 | 7.40 |
| CHEMBL143996 | — | — | 1 | 7.22 |
| CHEMBL274447 | — | — | 1 | 7.00 |
| CHEMBL342726 | — | — | 1 | 6.95 |
| CHEMBL423930 | — | — | 1 | 6.83 |
| CHEMBL423021 | — | — | 1 | 6.74 |
| CHEMBL277003 | — | — | 1 | 6.58 |
| CHEMBL343840 | — | — | 1 | 6.58 |
| CHEMBL145249 | — | — | 1 | 6.42 |
| CHEMBL343249 | — | — | 1 | 6.40 |
| CHEMBL343439 | — | — | 1 | 5.96 |
| CHEMBL146164 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL342553 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL255111 | — | Ki | = | 1.27 | nM | 8.90 |
| CHEMBL429847 | MILFASARTAN | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL344093 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL144016 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL358121 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL191 | LOSARTAN | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL144856 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL144764 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL142979 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL144646 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL143996 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL274447 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL342726 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL423930 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL423021 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL277003 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL343840 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL145249 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL343249 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL343439 | — | Ki | = | 1097.0 | nM | 5.96 |
| CHEMBL146164 | — | Ki | = | 5137.0 | nM | 5.29 |