Assay Detail
Binding
CHEMBL642988
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Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
N6-(arylalkyl)adenosines. Identification of N6-(9-fluorenylmethyl)adenosine as a highly potent agonist for the adenosine A2 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.39 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.92 |
| CHEMBL2181971 | — | — | 1 | 8.29 |
| CHEMBL464859 | NECA | — | 1 | 8.20 |
| CHEMBL193692 | — | — | 1 | 8.17 |
| CHEMBL285819 | — | — | 1 | 8.03 |
| CHEMBL604617 | — | — | 1 | 7.91 |
| CHEMBL1257013 | — | — | 1 | 7.89 |
| CHEMBL132960 | — | — | 1 | 7.62 |
| CHEMBL604967 | — | — | 1 | 7.21 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.92 |
| CHEMBL609501 | — | — | 1 | 6.80 |
| CHEMBL609790 | — | — | 1 | 6.50 |
| CHEMBL1256672 | — | — | 1 | 6.23 |
| CHEMBL604961 | — | — | 1 | 5.21 |
| CHEMBL606227 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL139000 | (R)-PIA | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2181971 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL464859 | NECA | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL193692 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL285819 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL604617 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL1257013 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL132960 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL604967 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL609501 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL609790 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL1256672 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL604961 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL606227 | — | Ki | = | 9000.0 | nM | 5.05 |