Assay Detail
Binding
CHEMBL643480
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Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the presence of GTP.
11
Total Activities
10
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
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 | 6.50 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 2 | 7.45 |
| CHEMBL477444 | — | — | 1 | 7.21 |
| CHEMBL263643 | — | — | 1 | 6.89 |
| CHEMBL2113469 | — | — | 1 | 6.83 |
| CHEMBL2113471 | — | — | 1 | 6.78 |
| CHEMBL2113468 | — | — | 1 | 6.70 |
| CHEMBL2113467 | — | — | 1 | 6.65 |
| CHEMBL2113470 | — | — | 1 | 5.58 |
| CHEMBL2113466 | — | — | 1 | 5.07 |
| CHEMBL2113472 | — | — | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 35.2 | nM | 7.45 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 35.2 | nM | 7.45 |
| CHEMBL477444 | — | Ki | = | 61.5 | nM | 7.21 |
| CHEMBL263643 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2113469 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL2113471 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL2113468 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL2113467 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL2113470 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL2113466 | — | Ki | = | 8560.0 | nM | 5.07 |
| CHEMBL2113472 | — | Ki | = | 14300.0 | nM | 4.84 |