Assay Detail
Binding
CHEMBL2072275
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Displacement of 3[H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cells after 60 mins by Liquid scintillation analysis
9
Total Activities
9
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
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 | 9 | 6.71 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070507 | — | — | 1 | 7.47 |
| CHEMBL464859 | NECA | — | 1 | 7.46 |
| CHEMBL261482 | — | — | 1 | 7.30 |
| CHEMBL2070398 | — | — | 1 | 6.75 |
| CHEMBL1235128 | — | — | 1 | 6.68 |
| CHEMBL1234591 | — | — | 1 | 6.30 |
| CHEMBL2070508 | — | — | 1 | 6.19 |
| CHEMBL129903 | — | — | 1 | 5.51 |
| CHEMBL2070506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070507 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL464859 | NECA | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL261482 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2070398 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1235128 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL1234591 | — | Ki | = | 505.0 | nM | 6.30 |
| CHEMBL2070508 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL129903 | — | Ki | = | 3120.0 | nM | 5.51 |
| CHEMBL2070506 | — | Ki | > | 10000.0 | nM | - |