Assay Detail
Binding
CHEMBL2399765
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Antagonist activity at angiotensin-2 receptor in Wistar rat endothelium denuded thoracic aorta assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior to angiotensin 2-challenge
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Thoracic aorta |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1- and AII-receptors antagonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 7.41 | 10.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2397829 | — | — | 1 | 10.64 |
| CHEMBL2397828 | — | — | 1 | 9.04 |
| CHEMBL2397833 | — | — | 1 | 8.83 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 8.43 |
| CHEMBL2397825 | — | — | 1 | 8.37 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 8.26 |
| CHEMBL2397824 | — | — | 1 | 7.65 |
| CHEMBL2397827 | — | — | 1 | 7.64 |
| CHEMBL2397837 | — | — | 1 | 7.41 |
| CHEMBL2397826 | — | — | 1 | 7.07 |
| CHEMBL2397835 | — | — | 1 | 7.03 |
| CHEMBL2397834 | — | — | 1 | 6.65 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 6.39 |
| CHEMBL2397836 | — | — | 1 | 6.14 |
| CHEMBL2397830 | — | — | 1 | 5.75 |
| CHEMBL2397832 | — | — | 1 | 5.52 |
| CHEMBL2397831 | — | — | 1 | 5.08 |
| CHEMBL511930 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2397829 | — | Kd | = | 0.02291 | nM | 10.64 |
| CHEMBL2397828 | — | Kd | = | 0.912 | nM | 9.04 |
| CHEMBL2397833 | — | Kd | = | 1.479 | nM | 8.83 |
| CHEMBL191 | LOSARTAN | Kd | = | 3.715 | nM | 8.43 |
| CHEMBL2397825 | — | Kd | = | 4.266 | nM | 8.37 |
| CHEMBL2 | PRAZOSIN | Kd | = | 5.495 | nM | 8.26 |
| CHEMBL2397824 | — | Kd | = | 22.39 | nM | 7.65 |
| CHEMBL2397827 | — | Kd | = | 22.91 | nM | 7.64 |
| CHEMBL2397837 | — | Kd | = | 38.9 | nM | 7.41 |
| CHEMBL2397826 | — | Kd | = | 85.11 | nM | 7.07 |
| CHEMBL2397835 | — | Kd | = | 93.33 | nM | 7.03 |
| CHEMBL2397834 | — | Kd | = | 223.87 | nM | 6.65 |
| CHEMBL611 | TERAZOSIN | Kd | = | 407.38 | nM | 6.39 |
| CHEMBL2397836 | — | Kd | = | 724.44 | nM | 6.14 |
| CHEMBL2397830 | — | Kd | = | 1778.28 | nM | 5.75 |
| CHEMBL2397832 | — | Kd | = | 3019.95 | nM | 5.52 |
| CHEMBL2397831 | — | Kd | = | 8317.64 | nM | 5.08 |
| CHEMBL511930 | — | Kd | = | 489778.82 | nM | - |