Assay Detail
Functional
CHEMBL886097
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at AT1 receptor assessed inhibition of angiotensin-2-induced contraction of rabbit thoracic aortic rings
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 13 | 7.52 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400424 | — | — | 1 | 8.50 |
| CHEMBL245444 | — | — | 1 | 8.40 |
| CHEMBL241523 | — | — | 1 | 8.20 |
| CHEMBL239378 | — | — | 1 | 8.00 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.90 |
| CHEMBL245644 | — | — | 1 | 7.90 |
| CHEMBL241685 | — | — | 1 | 7.80 |
| CHEMBL241684 | — | — | 1 | 7.50 |
| CHEMBL440051 | — | — | 1 | 7.10 |
| CHEMBL393305 | — | — | 1 | 7.00 |
| CHEMBL392118 | — | — | 1 | 7.00 |
| CHEMBL241529 | — | — | 1 | 6.50 |
| CHEMBL442251 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400424 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL245444 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL241523 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL239378 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL191 | LOSARTAN | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL245644 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL241685 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL241684 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL440051 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL393305 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL392118 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL241529 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL442251 | — | Kd | = | 1258.93 | nM | 5.90 |