Assay Detail
Binding
CHEMBL641038
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Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 12 | 8.10 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.49 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | — | 1 | 9.34 |
| CHEMBL45891 | — | — | 1 | 9.07 |
| CHEMBL2113423 | — | — | 1 | 8.68 |
| CHEMBL262083 | N6-PHENYLADENOSINE | — | 1 | 8.49 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 8.29 |
| CHEMBL262984 | — | — | 1 | 8.16 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.89 |
| CHEMBL337073 | — | — | 1 | 7.49 |
| CHEMBL340019 | — | — | 1 | 7.22 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.90 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL45891 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL2113423 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL262083 | N6-PHENYLADENOSINE | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL477 | ADENOSINE | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL262984 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL337073 | — | Ki | = | 32.6 | nM | 7.49 |
| CHEMBL340019 | — | Ki | = | 60.7 | nM | 7.22 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 700.0 | nM | 6.16 |