Assay Detail
Binding
CHEMBL1024509
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Displacement of [3H]CGS21680 from human recombinant adenosine A2a receptor expressed in HEK293 cells by liquid scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 5.79 | 6.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200732 | — | — | 1 | 6.65 |
| CHEMBL413686 | — | — | 1 | 6.47 |
| CHEMBL549352 | — | — | 1 | 6.00 |
| CHEMBL561855 | — | — | 1 | 5.85 |
| CHEMBL564676 | — | — | 1 | 5.47 |
| CHEMBL549563 | — | — | 1 | 5.44 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 5.27 |
| CHEMBL564883 | — | — | 1 | 5.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200732 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL413686 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL549352 | — | Ki | = | 997.0 | nM | 6.00 |
| CHEMBL561855 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL564676 | — | Ki | = | 3410.0 | nM | 5.47 |
| CHEMBL549563 | — | Ki | = | 3630.0 | nM | 5.44 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL564883 | — | Ki | = | 6560.0 | nM | 5.18 |