Assay Detail
Binding
CHEMBL881273
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Binding affinity against Adenosine A2A receptor using [3H]-CGS- 21680 as the radioligand in rat striatal membranes
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.03 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 2 | 6.24 |
| CHEMBL477444 | — | — | 1 | 5.06 |
| CHEMBL2113469 | — | — | 1 | 4.99 |
| CHEMBL2113471 | — | — | 1 | 4.95 |
| CHEMBL2113468 | — | — | 1 | 4.87 |
| CHEMBL2113472 | — | — | 1 | 4.84 |
| CHEMBL2113467 | — | — | 1 | 4.73 |
| CHEMBL263643 | — | — | 1 | 4.72 |
| CHEMBL2113466 | — | — | 1 | 4.37 |
| CHEMBL2113470 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL477444 | — | Ki | = | 8750.0 | nM | 5.06 |
| CHEMBL2113469 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL2113471 | — | Ki | = | 11300.0 | nM | 4.95 |
| CHEMBL2113468 | — | Ki | = | 13500.0 | nM | 4.87 |
| CHEMBL2113472 | — | Ki | = | 14500.0 | nM | 4.84 |
| CHEMBL2113467 | — | Ki | = | 18800.0 | nM | 4.73 |
| CHEMBL263643 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL2113466 | — | Ki | = | 42500.0 | nM | 4.37 |
| CHEMBL2113470 | — | Ki | = | 45500.0 | nM | 4.34 |