Assay Detail
Functional
CHEMBL772135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against [125I]angiotensin II(AII) induced contraction in rabbit aorta by 50%
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
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 | 39 | 7.33 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 8.74 |
| CHEMBL309089 | — | — | 1 | 8.63 |
| CHEMBL76166 | — | — | 1 | 8.59 |
| CHEMBL306259 | — | — | 1 | 8.54 |
| CHEMBL308261 | — | — | 1 | 8.48 |
| CHEMBL307844 | — | — | 1 | 8.42 |
| CHEMBL70371 | — | — | 1 | 8.40 |
| CHEMBL76169 | — | — | 1 | 8.35 |
| CHEMBL308031 | — | — | 1 | 8.32 |
| CHEMBL72922 | — | — | 1 | 8.27 |
| CHEMBL306066 | — | — | 1 | 8.15 |
| CHEMBL73084 | — | — | 1 | 8.05 |
| CHEMBL73433 | — | — | 1 | 7.75 |
| CHEMBL306949 | — | — | 1 | 7.72 |
| CHEMBL308779 | — | — | 1 | 7.68 |
| CHEMBL306612 | — | — | 1 | 7.47 |
| CHEMBL307432 | — | — | 1 | 7.41 |
| CHEMBL275652 | — | — | 1 | 7.28 |
| CHEMBL72453 | — | — | 1 | 7.24 |
| CHEMBL76393 | — | — | 1 | 7.15 |
| CHEMBL306852 | — | — | 1 | 7.14 |
| CHEMBL307455 | — | — | 1 | 7.09 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.05 |
| CHEMBL308961 | — | — | 1 | 6.82 |
| CHEMBL73646 | — | — | 1 | 6.48 |
| CHEMBL75498 | — | — | 1 | 6.40 |
| CHEMBL431390 | — | — | 1 | 6.37 |
| CHEMBL73564 | — | — | 1 | 6.11 |
| CHEMBL72080 | — | — | 1 | 5.82 |
| CHEMBL73358 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL309089 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL76166 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL306259 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL308261 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL307844 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL70371 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL76169 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL308031 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL72922 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL306066 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL73084 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL73433 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL306949 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL308779 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL306612 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL307432 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL275652 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL72453 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL76393 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL306852 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL307455 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL191 | LOSARTAN | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL308961 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL73646 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL75498 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL431390 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL73564 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL72080 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL73358 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL73463 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL75935 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL307284 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL76330 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL312286 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL75518 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL309094 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL418893 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL75840 | — | IC50 | > | 100.0 | nM | - |