Assay Detail
Functional
CHEMBL648846
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 without using bovine serum albumin (BSA)
9
Total Activities
9
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 | 9 | 7.82 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87964 | — | — | 1 | 8.68 |
| CHEMBL422593 | — | — | 1 | 8.34 |
| CHEMBL87778 | — | — | 1 | 8.30 |
| CHEMBL314590 | — | — | 1 | 7.85 |
| CHEMBL315128 | — | — | 1 | 7.85 |
| CHEMBL87392 | — | — | 1 | 7.68 |
| CHEMBL85704 | — | — | 1 | 7.30 |
| CHEMBL86143 | — | — | 1 | 7.30 |
| CHEMBL313017 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87964 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL422593 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL87778 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL314590 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL315128 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL87392 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL85704 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL86143 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL313017 | — | IC50 | = | 90.0 | nM | 7.05 |