Assay Detail
Binding
CHEMBL641316
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Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.37 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66393 | — | — | 1 | 7.76 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.52 |
| CHEMBL307199 | — | — | 1 | 7.42 |
| CHEMBL284969 | — | — | 1 | 6.22 |
| CHEMBL417292 | — | — | 1 | 6.22 |
| CHEMBL27809 | — | — | 1 | 6.13 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.07 |
| CHEMBL49935 | ARISTEROMYCIN | — | 1 | 5.67 |
| CHEMBL284216 | — | — | 1 | 5.47 |
| CHEMBL27952 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66393 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL477 | ADENOSINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL307199 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL284969 | — | Ki | = | 605.0 | nM | 6.22 |
| CHEMBL417292 | — | Ki | = | 601.0 | nM | 6.22 |
| CHEMBL27809 | — | Ki | = | 732.0 | nM | 6.13 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 857.0 | nM | 6.07 |
| CHEMBL49935 | ARISTEROMYCIN | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL284216 | — | Ki | = | 3390.0 | nM | 5.47 |
| CHEMBL27952 | — | Ki | = | 6800.0 | nM | 5.17 |