Assay Detail
Binding
CHEMBL640528
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[3H]NECA saturation binding in CHO cells expressing human recombinant A2A adenosine receptor
5
Total Activities
5
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 | Expert |
Publication
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.08 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.70 |
| CHEMBL61259 | — | — | 1 | 6.22 |
| CHEMBL3350496 | — | — | 1 | 4.33 |
| CHEMBL2181966 | — | — | 1 | - |
| CHEMBL3350497 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL61259 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3350496 | — | Ki | = | 46600.0 | nM | 4.33 |
| CHEMBL2181966 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3350497 | — | Ki | > | 100000.0 | nM | - |