Assay Detail
Binding
CHEMBL2174889
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Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.84 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 8.74 |
| CHEMBL464859 | NECA | — | 1 | 8.17 |
| CHEMBL1512545 | — | — | 1 | 7.98 |
| CHEMBL2012686 | — | — | 1 | 7.32 |
| CHEMBL2170795 | — | — | 1 | 7.25 |
| CHEMBL2012684 | — | — | 1 | 7.17 |
| CHEMBL2170785 | — | — | 1 | 7.17 |
| CHEMBL2170787 | — | — | 1 | 7.12 |
| CHEMBL2012685 | — | — | 1 | 7.06 |
| CHEMBL2170790 | — | — | 1 | 6.92 |
| CHEMBL2170786 | — | — | 1 | 6.82 |
| CHEMBL2170788 | — | — | 1 | 6.82 |
| CHEMBL2170792 | — | — | 1 | 6.77 |
| CHEMBL2170797 | — | — | 1 | 6.68 |
| CHEMBL2170789 | — | — | 1 | 6.57 |
| CHEMBL2012672 | — | — | 1 | 6.46 |
| CHEMBL2170791 | — | — | 1 | 6.31 |
| CHEMBL2170796 | — | — | 1 | 6.31 |
| CHEMBL2170798 | — | — | 1 | 6.14 |
| CHEMBL2170800 | — | — | 1 | 6.11 |
| CHEMBL2012680 | — | — | 1 | 6.03 |
| CHEMBL2170799 | — | — | 1 | 5.97 |
| CHEMBL2170793 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL464859 | NECA | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL1512545 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL2012686 | — | Ki | = | 47.9 | nM | 7.32 |
| CHEMBL2170795 | — | Ki | = | 56.1 | nM | 7.25 |
| CHEMBL2012684 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL2170785 | — | Ki | = | 68.1 | nM | 7.17 |
| CHEMBL2170787 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL2012685 | — | Ki | = | 86.8 | nM | 7.06 |
| CHEMBL2170790 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2170786 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2170788 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2170792 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2170797 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2170789 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2012672 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL2170791 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL2170796 | — | Ki | = | 488.0 | nM | 6.31 |
| CHEMBL2170798 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL2170800 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL2012680 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL2170799 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL2170793 | — | Ki | = | 3000.0 | nM | 5.52 |