Assay Detail
Binding
CHEMBL2174887
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Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 17 | 5.68 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.70 |
| CHEMBL1512545 | — | — | 1 | 6.43 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.10 |
| CHEMBL2170787 | — | — | 1 | 5.80 |
| CHEMBL2170796 | — | — | 1 | 5.65 |
| CHEMBL284969 | — | — | 1 | 5.64 |
| CHEMBL2170792 | — | — | 1 | 5.59 |
| CHEMBL2012672 | — | — | 1 | 5.50 |
| CHEMBL2170788 | — | — | 1 | 5.44 |
| CHEMBL2170785 | — | — | 1 | 5.44 |
| CHEMBL2012686 | — | — | 1 | 5.40 |
| CHEMBL2170798 | — | — | 1 | 5.39 |
| CHEMBL2012684 | — | — | 1 | 5.36 |
| CHEMBL2170791 | — | — | 1 | 5.32 |
| CHEMBL2170786 | — | — | 1 | 5.31 |
| CHEMBL2170789 | — | — | 1 | 5.26 |
| CHEMBL2170790 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1512545 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL2170787 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL2170796 | — | Ki | = | 2230.0 | nM | 5.65 |
| CHEMBL284969 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL2170792 | — | Ki | = | 2550.0 | nM | 5.59 |
| CHEMBL2012672 | — | Ki | = | 3140.0 | nM | 5.50 |
| CHEMBL2170788 | — | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL2170785 | — | Ki | = | 3610.0 | nM | 5.44 |
| CHEMBL2012686 | — | Ki | = | 3950.0 | nM | 5.40 |
| CHEMBL2170798 | — | Ki | = | 4110.0 | nM | 5.39 |
| CHEMBL2012684 | — | Ki | = | 4410.0 | nM | 5.36 |
| CHEMBL2170791 | — | Ki | = | 4840.0 | nM | 5.32 |
| CHEMBL2170786 | — | Ki | = | 4910.0 | nM | 5.31 |
| CHEMBL2170789 | — | Ki | = | 5470.0 | nM | 5.26 |
| CHEMBL2170790 | — | Ki | = | 6450.0 | nM | 5.19 |