Assay Detail
Binding
CHEMBL641297
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Binding affinity for adenosine A2A receptor as displacement of [3H]-CGS- 21680 from rat striatal membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 4.75 | 5.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL108753 | — | — | 1 | 5.62 |
| CHEMBL2112484 | — | — | 1 | 5.14 |
| CHEMBL105764 | — | — | 1 | 4.66 |
| CHEMBL321178 | — | — | 1 | 4.64 |
| CHEMBL322332 | — | — | 1 | 4.56 |
| CHEMBL107155 | — | — | 1 | 4.54 |
| CHEMBL100071 | — | — | 1 | 4.45 |
| CHEMBL108797 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL108753 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL2112484 | — | Ki | = | 7160.0 | nM | 5.14 |
| CHEMBL105764 | — | Ki | = | 21800.0 | nM | 4.66 |
| CHEMBL321178 | — | Ki | = | 22900.0 | nM | 4.64 |
| CHEMBL322332 | — | Ki | = | 27600.0 | nM | 4.56 |
| CHEMBL107155 | — | Ki | = | 28900.0 | nM | 4.54 |
| CHEMBL100071 | — | Ki | = | 35900.0 | nM | 4.45 |
| CHEMBL108797 | — | Ki | = | 43000.0 | nM | 4.37 |