Assay Detail
Binding
CHEMBL648848
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In vitro binding affinity determined by its ability to displace the specific binding ligand [125I]-Sar1, Ile8-AII from Angiotensin II receptor, type 1 in rabbit aorta membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Imidazo[4,5-b]pyridine-based AT1 / AT2 angiotensin II receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 9.22 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68638 | — | — | 1 | 10.00 |
| CHEMBL304947 | — | — | 1 | 10.00 |
| CHEMBL306407 | — | — | 1 | 9.96 |
| CHEMBL68618 | — | — | 1 | 9.92 |
| CHEMBL304946 | — | — | 1 | 9.59 |
| CHEMBL71388 | — | — | 1 | 9.57 |
| CHEMBL7550 | L-158809 | — | 1 | 9.52 |
| CHEMBL302519 | — | — | 1 | 9.48 |
| CHEMBL67801 | — | — | 1 | 9.43 |
| CHEMBL71253 | — | — | 1 | 9.30 |
| CHEMBL67921 | — | — | 1 | 9.29 |
| CHEMBL71925 | — | — | 1 | 9.22 |
| CHEMBL448476 | — | — | 1 | 9.22 |
| CHEMBL307757 | — | — | 1 | 9.22 |
| CHEMBL296725 | — | — | 1 | 9.00 |
| CHEMBL302102 | — | — | 1 | 9.00 |
| CHEMBL68786 | — | — | 1 | 8.80 |
| CHEMBL308237 | — | — | 1 | 8.48 |
| CHEMBL306641 | — | — | 1 | 8.37 |
| CHEMBL308238 | — | — | 1 | 8.34 |
| CHEMBL67805 | — | — | 1 | 7.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68638 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL304947 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL306407 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL68618 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL304946 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL71388 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL7550 | L-158809 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL302519 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL67801 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL71253 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL67921 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL71925 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL448476 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL307757 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL296725 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL302102 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL68786 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL308237 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL306641 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL308238 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL67805 | — | IC50 | = | 11.5 | nM | 7.94 |