Assay Detail
Binding
CHEMBL642189
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Binding affinity against Adenosine A1 receptor using [3H]CHA in rat brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.20 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3038260 | — | — | 1 | 9.62 |
| CHEMBL2112182 | — | — | 1 | 9.52 |
| CHEMBL3038256 | — | — | 1 | 9.38 |
| CHEMBL489640 | — | — | 1 | 9.38 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL477444 | — | — | 1 | 9.14 |
| CHEMBL2112183 | — | — | 1 | 9.04 |
| CHEMBL2112184 | — | — | 1 | 8.78 |
| CHEMBL3038259 | — | — | 1 | 8.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3038260 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL2112182 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3038256 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL489640 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL477444 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL2112183 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL2112184 | — | Ki | = | 1.65 | nM | 8.78 |
| CHEMBL3038259 | — | Ki | = | 1.86 | nM | 8.73 |