Assay Detail
Binding
CHEMBL2072278
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Displacement of 3[H]CGS21680 from rat A2A adenosine receptor expressed in HEK293 cells after 60 min by Liquid scintillation analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.85 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.92 |
| CHEMBL261482 | — | — | 1 | 7.92 |
| CHEMBL2070398 | — | — | 1 | 6.39 |
| CHEMBL2070399 | — | — | 1 | 6.39 |
| CHEMBL1235128 | — | — | 1 | 6.26 |
| CHEMBL2070508 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL261482 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2070398 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL2070399 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL1235128 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2070508 | — | Ki | = | 610.0 | nM | 6.21 |