Assay Detail
Binding
CHEMBL643149
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Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
N6-cycloalkyladenosines. Potent, A1-selective adenosine agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.87 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL569275 | — | — | 1 | 9.11 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.94 |
| CHEMBL45891 | — | — | 1 | 8.88 |
| CHEMBL2113430 | — | — | 1 | 8.55 |
| CHEMBL2113424 | — | — | 1 | 8.39 |
| CHEMBL464859 | NECA | — | 1 | 8.21 |
| CHEMBL285819 | — | — | 1 | 8.06 |
| CHEMBL420705 | (S)-PIA | — | 1 | 7.32 |
| CHEMBL603382 | — | — | 1 | 7.00 |
| CHEMBL606090 | — | — | 1 | 6.84 |
| CHEMBL2113423 | — | — | 1 | 6.50 |
| CHEMBL604646 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL569275 | — | Ki | = | 0.777 | nM | 9.11 |
| CHEMBL139000 | (R)-PIA | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL45891 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL2113430 | — | Ki | = | 2.79 | nM | 8.55 |
| CHEMBL2113424 | — | Ki | = | 4.03 | nM | 8.39 |
| CHEMBL464859 | NECA | Ki | = | 6.24 | nM | 8.21 |
| CHEMBL285819 | — | Ki | = | 8.74 | nM | 8.06 |
| CHEMBL420705 | (S)-PIA | Ki | = | 47.6 | nM | 7.32 |
| CHEMBL603382 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL606090 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL2113423 | — | Ki | = | 319.0 | nM | 6.50 |
| CHEMBL604646 | — | Ki | = | 5390.0 | nM | 5.27 |