Assay Detail
Binding
CHEMBL640428
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Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.83 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1950647 | — | — | 1 | 8.24 |
| CHEMBL331372 | CGS-21680 | — | 1 | 7.82 |
| CHEMBL66393 | — | — | 1 | 7.76 |
| CHEMBL307199 | — | — | 1 | 7.42 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.25 |
| CHEMBL285819 | — | — | 1 | 7.20 |
| CHEMBL2113561 | — | — | 1 | 6.93 |
| CHEMBL1256714 | — | — | 1 | 6.76 |
| CHEMBL133566 | — | — | 1 | 6.71 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.33 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.33 |
| CHEMBL284969 | — | — | 1 | 6.02 |
| CHEMBL2113557 | — | — | 1 | 5.49 |
| CHEMBL2113562 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1950647 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL331372 | CGS-21680 | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL66393 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL307199 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL119709 | IB-MECA | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL285819 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2113561 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL1256714 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL133566 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 462.0 | nM | 6.33 |
| CHEMBL284969 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL2113557 | — | Ki | = | 3210.0 | nM | 5.49 |
| CHEMBL2113562 | — | Ki | = | 4120.0 | nM | 5.38 |