Assay Detail
Binding
CHEMBL648852
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 125I[Sar,Ile] from rabbit aorta membrane Angiotensin II receptor type 1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Triazolinones as nonpeptide angiotensin II antagonists. 2. discovery of a potent and orally active triazolinone acylsulfonamide
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.79 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL279629 | L-159913 | — | 1 | 9.37 |
| CHEMBL19018 | — | — | 1 | 9.11 |
| CHEMBL278305 | — | — | 1 | 9.10 |
| CHEMBL278977 | — | — | 1 | 9.10 |
| CHEMBL275160 | — | — | 1 | 8.85 |
| CHEMBL274710 | — | — | 1 | 8.80 |
| CHEMBL19202 | — | — | 1 | 8.68 |
| CHEMBL18287 | — | — | 1 | 8.62 |
| CHEMBL18606 | — | — | 1 | 8.59 |
| CHEMBL274712 | — | — | 1 | 8.54 |
| CHEMBL429058 | — | — | 1 | 8.48 |
| CHEMBL278741 | — | — | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL279629 | L-159913 | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL19018 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL278305 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL278977 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL275160 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL274710 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL19202 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL18287 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL18606 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL274712 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL429058 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL278741 | — | IC50 | = | 5.8 | nM | 8.24 |