Assay Detail
Binding
CHEMBL640781
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Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor
12
Total Activities
12
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
Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.68 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL1512545 | — | — | 1 | 9.07 |
| CHEMBL2092973 | — | — | 1 | 8.92 |
| CHEMBL45891 | — | — | 1 | 8.89 |
| CHEMBL285819 | — | — | 1 | 8.03 |
| CHEMBL610099 | — | — | 1 | 8.03 |
| CHEMBL464859 | NECA | — | 1 | 7.99 |
| CHEMBL610435 | — | — | 1 | 7.39 |
| CHEMBL2364548 | — | — | 1 | 7.13 |
| CHEMBL2113576 | — | — | 1 | 6.21 |
| CHEMBL1788287 | — | — | 1 | 5.74 |
| CHEMBL331372 | CGS-21680 | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL1512545 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL2092973 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL45891 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL285819 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL610099 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL464859 | NECA | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL610435 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL2364548 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL2113576 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL1788287 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL331372 | CGS-21680 | Ki | = | 2600.0 | nM | 5.58 |