Assay Detail
Binding
CHEMBL646486
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Binding of Adenosine A2 receptor in whole rat brain membrane using [3H]CHA as a Radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.31 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 8.96 |
| CHEMBL45891 | — | — | 1 | 8.62 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | — | 1 | 8.41 |
| CHEMBL321505 | — | — | 1 | 8.33 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.68 |
| CHEMBL262083 | N6-PHENYLADENOSINE | — | 1 | 6.96 |
| CHEMBL262984 | — | — | 1 | 6.80 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.46 |
| CHEMBL337073 | — | — | 1 | 6.19 |
| CHEMBL340019 | — | — | 1 | 6.07 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL45891 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL321505 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL262083 | N6-PHENYLADENOSINE | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL262984 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL337073 | — | Ki | = | 644.0 | nM | 6.19 |
| CHEMBL340019 | — | Ki | = | 848.0 | nM | 6.07 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 1310.0 | nM | 5.88 |