Assay Detail
Functional
CHEMBL853543
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscle
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pA2 | 17 | - | - |
| Kd | 6 | 6.69 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382135 | — | — | 1 | 7.36 |
| CHEMBL199446 | — | — | 1 | 7.29 |
| CHEMBL370378 | — | — | 1 | 6.90 |
| CHEMBL372148 | — | — | 1 | 6.33 |
| CHEMBL201721 | — | — | 1 | 6.20 |
| CHEMBL201750 | — | — | 1 | 6.03 |
| CHEMBL199910 | — | — | 1 | - |
| CHEMBL199717 | — | — | 1 | - |
| CHEMBL201003 | — | — | 1 | - |
| CHEMBL197606 | — | — | 1 | - |
| CHEMBL199808 | — | — | 1 | - |
| CHEMBL203208 | — | — | 1 | - |
| CHEMBL199856 | — | — | 1 | - |
| CHEMBL201608 | — | — | 1 | - |
| CHEMBL203467 | — | — | 1 | - |
| CHEMBL201217 | — | — | 1 | - |
| CHEMBL201228 | — | — | 1 | - |
| CHEMBL201591 | — | — | 1 | - |
| CHEMBL381747 | — | — | 1 | - |
| CHEMBL201578 | — | — | 1 | - |
| CHEMBL201536 | — | — | 1 | - |
| CHEMBL202925 | — | — | 1 | - |
| CHEMBL383031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382135 | — | Kd | = | 43.65 | nM | 7.36 |
| CHEMBL199446 | — | Kd | = | 51.29 | nM | 7.29 |
| CHEMBL370378 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL372148 | — | Kd | = | 467.74 | nM | 6.33 |
| CHEMBL201721 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL201750 | — | Kd | = | 933.25 | nM | 6.03 |
| CHEMBL199910 | — | pA2 | - | — | - | |
| CHEMBL199717 | — | pA2 | - | — | - | |
| CHEMBL201003 | — | pA2 | - | — | - | |
| CHEMBL197606 | — | pA2 | - | — | - | |
| CHEMBL199808 | — | pA2 | - | — | - | |
| CHEMBL203208 | — | pA2 | - | — | - | |
| CHEMBL199856 | — | pA2 | - | — | - | |
| CHEMBL201608 | — | pA2 | - | — | - | |
| CHEMBL203467 | — | pA2 | - | — | - | |
| CHEMBL201217 | — | pA2 | - | — | - | |
| CHEMBL201228 | — | pA2 | - | — | - | |
| CHEMBL201591 | — | pA2 | - | — | - | |
| CHEMBL381747 | — | pA2 | - | — | - | |
| CHEMBL201578 | — | pA2 | - | — | - | |
| CHEMBL201536 | — | pA2 | - | — | - | |
| CHEMBL202925 | — | pA2 | - | — | - | |
| CHEMBL383031 | — | pA2 | - | — | - |