Assay Detail
Functional
CHEMBL940082
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Antagonist activity at adenosine A2A receptor in Sprague-Dawley rat aorta smooth muscle
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 6.25 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262332 | — | — | 1 | 6.80 |
| CHEMBL259580 | — | — | 1 | 6.63 |
| CHEMBL407179 | — | — | 1 | 6.40 |
| CHEMBL259105 | — | — | 1 | 6.30 |
| CHEMBL294223 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262332 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL259580 | — | Kd | = | 234.42 | nM | 6.63 |
| CHEMBL407179 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL259105 | — | Kd | = | 501.19 | nM | 6.30 |
| CHEMBL294223 | — | Kd | = | 7943.28 | nM | 5.10 |