Assay Detail
Functional
CHEMBL652728
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 1
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 8.32 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL329616 | — | — | 1 | 9.74 |
| CHEMBL433646 | — | — | 1 | 9.70 |
| CHEMBL120199 | — | — | 1 | 9.62 |
| CHEMBL92654 | — | — | 1 | 9.62 |
| CHEMBL93226 | — | — | 1 | 9.46 |
| CHEMBL334145 | — | — | 1 | 9.38 |
| CHEMBL90011 | — | — | 1 | 9.34 |
| CHEMBL90774 | — | — | 1 | 9.30 |
| CHEMBL281386 | — | — | 1 | 9.28 |
| CHEMBL332897 | — | — | 1 | 9.26 |
| CHEMBL92472 | — | — | 1 | 9.22 |
| CHEMBL93886 | — | — | 1 | 9.19 |
| CHEMBL120457 | — | — | 1 | 9.17 |
| CHEMBL338740 | — | — | 1 | 9.16 |
| CHEMBL94002 | — | — | 1 | 9.11 |
| CHEMBL333800 | — | — | 1 | 9.10 |
| CHEMBL443269 | — | — | 1 | 8.96 |
| CHEMBL94221 | — | — | 1 | 8.89 |
| CHEMBL333978 | — | — | 1 | 8.80 |
| CHEMBL123767 | — | — | 1 | 8.77 |
| CHEMBL93547 | — | — | 1 | 8.77 |
| CHEMBL283975 | — | — | 1 | 8.70 |
| CHEMBL334192 | — | — | 1 | 8.68 |
| CHEMBL330571 | — | — | 1 | 8.64 |
| CHEMBL121416 | — | — | 1 | 8.60 |
| CHEMBL431887 | — | — | 1 | 8.57 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 8.55 |
| CHEMBL327982 | — | — | 1 | 8.54 |
| CHEMBL315878 | — | — | 1 | 8.49 |
| CHEMBL121847 | — | — | 1 | 8.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL329616 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL433646 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL92654 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL120199 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL93226 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL334145 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL90011 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL90774 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL281386 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL332897 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL92472 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL93886 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL120457 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL338740 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL94002 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL333800 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL443269 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL94221 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL333978 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL123767 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL93547 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL283975 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL334192 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL330571 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL121416 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL431887 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL327982 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL315878 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL121847 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL331475 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL327837 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL120290 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL327718 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL93735 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL92821 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL121125 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL120750 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL331078 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL327862 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL120762 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL406791 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL118431 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL328598 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL191 | LOSARTAN | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL334083 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL93289 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL331063 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL331886 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL120549 | — | IC50 | = | 76.0 | nM | 7.12 |