Assay Detail
Binding
CHEMBL649502
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Inhibitory concentration against binding of [125I]angiotensin II to rat liver expressing Angiotensin II receptor
44
Total Activities
44
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
Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoroacetyl)-1H-pyrrol-1-yl]-1H- imidazole-5-carboxylic acid (CI-996).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 8.04 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308261 | — | — | 1 | 9.39 |
| CHEMBL307844 | — | — | 1 | 9.24 |
| CHEMBL76166 | — | — | 1 | 9.10 |
| CHEMBL309089 | — | — | 1 | 9.09 |
| CHEMBL76169 | — | — | 1 | 9.05 |
| CHEMBL306259 | — | — | 1 | 8.98 |
| CHEMBL72922 | — | — | 1 | 8.93 |
| CHEMBL307455 | — | — | 1 | 8.86 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 8.80 |
| CHEMBL306066 | — | — | 1 | 8.80 |
| CHEMBL70371 | — | — | 1 | 8.62 |
| CHEMBL73433 | — | — | 1 | 8.60 |
| CHEMBL308031 | — | — | 1 | 8.55 |
| CHEMBL75518 | — | — | 1 | 8.55 |
| CHEMBL308779 | — | — | 1 | 8.48 |
| CHEMBL275652 | — | — | 1 | 8.45 |
| CHEMBL306852 | — | — | 1 | 8.44 |
| CHEMBL431390 | — | — | 1 | 8.41 |
| CHEMBL306612 | — | — | 1 | 8.40 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 8.30 |
| CHEMBL75935 | — | — | 1 | 8.25 |
| CHEMBL72453 | — | — | 1 | 8.06 |
| CHEMBL73084 | — | — | 1 | 7.96 |
| CHEMBL306949 | — | — | 1 | 7.95 |
| CHEMBL73646 | — | — | 1 | 7.91 |
| CHEMBL76393 | — | — | 1 | 7.86 |
| CHEMBL309094 | — | — | 1 | 7.82 |
| CHEMBL76330 | — | — | 1 | 7.73 |
| CHEMBL308961 | — | — | 1 | 7.68 |
| CHEMBL73725 | — | — | 1 | 7.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308261 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL307844 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL76166 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL309089 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL76169 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL306259 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL72922 | — | IC50 | = | 1.17 | nM | 8.93 |
| CHEMBL307455 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL306066 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL70371 | — | IC50 | = | 2.37 | nM | 8.62 |
| CHEMBL73433 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL308031 | — | IC50 | = | 2.81 | nM | 8.55 |
| CHEMBL75518 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL308779 | — | IC50 | = | 3.32 | nM | 8.48 |
| CHEMBL275652 | — | IC50 | = | 3.57 | nM | 8.45 |
| CHEMBL306852 | — | IC50 | = | 3.64 | nM | 8.44 |
| CHEMBL431390 | — | IC50 | = | 3.93 | nM | 8.41 |
| CHEMBL306612 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL191 | LOSARTAN | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL75935 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL72453 | — | IC50 | = | 8.76 | nM | 8.06 |
| CHEMBL73084 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL306949 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL73646 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL76393 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL309094 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL76330 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL308961 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL73725 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL75092 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL307284 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL307432 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL306750 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL75498 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL73463 | — | IC50 | = | 53.3 | nM | 7.27 |
| CHEMBL75840 | — | IC50 | = | 65.5 | nM | 7.18 |
| CHEMBL72361 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL312286 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL73564 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL420198 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL418893 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL73358 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL72080 | — | IC50 | = | 332.0 | nM | 6.48 |