Assay Detail
Binding
CHEMBL642299
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Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes
11
Total Activities
11
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
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.02 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.10 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.89 |
| CHEMBL2113390 | — | — | 1 | 8.80 |
| CHEMBL2113389 | — | — | 1 | 8.12 |
| CHEMBL606016 | — | — | 1 | 8.11 |
| CHEMBL464859 | NECA | — | 1 | 8.09 |
| CHEMBL2113387 | — | — | 1 | 7.80 |
| CHEMBL605008 | — | — | 1 | 7.75 |
| CHEMBL2113391 | — | — | 1 | 7.33 |
| CHEMBL2113396 | — | — | 1 | 7.29 |
| CHEMBL115824 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL139000 | (R)-PIA | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2113390 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2113389 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL606016 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL464859 | NECA | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL2113387 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL605008 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2113391 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2113396 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL115824 | — | Ki | = | 115.0 | nM | 6.94 |