Assay Detail
Functional
CHEMBL853544
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus |
| Confidence | 8 — Homologous 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 | 8.09 | 8.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370378 | — | — | 1 | 8.53 |
| CHEMBL201750 | — | — | 1 | 8.26 |
| CHEMBL199446 | — | — | 1 | 8.25 |
| CHEMBL382135 | — | — | 1 | 8.10 |
| CHEMBL372148 | — | — | 1 | 8.09 |
| CHEMBL201721 | — | — | 1 | 7.28 |
| 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 |
|---|---|---|---|---|---|---|
| CHEMBL370378 | — | Kd | = | 2.951 | nM | 8.53 |
| CHEMBL201750 | — | Kd | = | 5.495 | nM | 8.26 |
| CHEMBL199446 | — | Kd | = | 5.623 | nM | 8.25 |
| CHEMBL382135 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL372148 | — | Kd | = | 8.128 | nM | 8.09 |
| CHEMBL201721 | — | Kd | = | 52.48 | nM | 7.28 |
| 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 | - | — | - |