Assay Detail
Functional
CHEMBL1669992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at angiotensin AT1 receptor in rabbit aorta
18
Total Activities
18
Compounds Tested
6
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 12 | 9.08 | 10.30 |
| IC50 | 2 | 9.54 | 9.70 |
| pKb | 1 | - | - |
| pD2 | 1 | - | - |
| Kb | 1 | - | - |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293511 | — | — | 1 | 10.30 |
| CHEMBL418226 | — | — | 1 | 10.30 |
| CHEMBL416477 | — | — | 1 | 10.10 |
| CHEMBL41194 | PRATOSARTAN | 2.0 | 1 | 10.04 |
| CHEMBL49410 | — | — | 1 | 9.93 |
| CHEMBL288246 | — | — | 1 | 9.70 |
| CHEMBL334145 | — | — | 1 | 9.38 |
| CHEMBL48602 | — | — | 1 | 9.00 |
| CHEMBL347610 | — | — | 1 | 8.82 |
| CHEMBL71162 | — | — | 1 | 8.70 |
| CHEMBL158725 | — | — | 1 | 8.45 |
| CHEMBL284536 | — | — | 1 | 8.30 |
| CHEMBL275875 | CL-329167 | — | 1 | 8.01 |
| CHEMBL341716 | — | — | 1 | 7.00 |
| CHEMBL43591 | — | — | 1 | - |
| CHEMBL305544 | SAPRISARTAN | 2.0 | 1 | - |
| CHEMBL268004 | — | — | 1 | - |
| CHEMBL122638 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293511 | — | Kd | = | 0.05012 | nM | 10.30 |
| CHEMBL418226 | — | Kd | = | 0.05012 | nM | 10.30 |
| CHEMBL416477 | — | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL41194 | PRATOSARTAN | Kd | = | 0.0912 | nM | 10.04 |
| CHEMBL49410 | — | Kd | = | 0.1175 | nM | 9.93 |
| CHEMBL288246 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL334145 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL48602 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL347610 | — | Kd | = | 1.514 | nM | 8.82 |
| CHEMBL71162 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL158725 | — | Kd | = | 3.548 | nM | 8.45 |
| CHEMBL284536 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL275875 | CL-329167 | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL341716 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL43591 | — | pD2 | = | 9.91 | — | - |
| CHEMBL305544 | SAPRISARTAN | pKb | = | 9.0 | — | - |
| CHEMBL268004 | — | Kb | = | 0.08 | nM | - |
| CHEMBL122638 | — | Activity | = | 3.8 | nM | - |