Assay Detail
Functional
CHEMBL648845
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.96 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87778 | — | — | 1 | 8.74 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.72 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87778 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL191 | LOSARTAN | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | IC50 | = | 37.0 | nM | 7.43 |