Assay Detail
Binding
CHEMBL888474
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Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells
9
Total Activities
9
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 | Expert |
Publication
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 5.92 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388145 | — | — | 1 | 7.35 |
| CHEMBL200732 | — | — | 1 | 6.65 |
| CHEMBL413686 | — | — | 1 | 6.47 |
| CHEMBL227279 | — | — | 1 | 5.80 |
| CHEMBL437923 | — | — | 1 | 5.40 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 5.27 |
| CHEMBL344187 | — | — | 1 | 4.53 |
| CHEMBL436485 | — | — | 1 | - |
| CHEMBL373065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388145 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL200732 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL413686 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL227279 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL437923 | — | Ki | = | 4020.0 | nM | 5.40 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 5360.0 | nM | 5.27 |
| CHEMBL344187 | — | Ki | = | 29800.0 | nM | 4.53 |
| CHEMBL436485 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL373065 | — | Ki | > | 10000.0 | nM | - |