Assay Detail
Binding
CHEMBL647735
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Displacement of [3H]-CGH 21680 from Adenosine A2A receptor of rat striatal membranes
13
Total Activities
13
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
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.83 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95811 | — | — | 1 | 7.84 |
| CHEMBL318251 | — | — | 1 | 7.44 |
| CHEMBL319971 | — | — | 1 | 7.42 |
| CHEMBL313422 | — | — | 1 | 7.31 |
| CHEMBL88147 | — | — | 1 | 7.28 |
| CHEMBL317310 | — | — | 1 | 7.05 |
| CHEMBL96041 | — | — | 1 | 7.04 |
| CHEMBL329722 | — | — | 1 | 6.97 |
| CHEMBL100195 | — | — | 1 | 6.87 |
| CHEMBL317382 | — | — | 1 | 6.56 |
| CHEMBL93932 | — | — | 1 | 6.51 |
| CHEMBL414023 | — | — | 1 | 5.36 |
| CHEMBL97383 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95811 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL318251 | — | Ki | = | 36.3 | nM | 7.44 |
| CHEMBL319971 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL313422 | — | Ki | = | 48.8 | nM | 7.31 |
| CHEMBL88147 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL317310 | — | Ki | = | 88.8 | nM | 7.05 |
| CHEMBL96041 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL329722 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL100195 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL317382 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL93932 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL414023 | — | Ki | = | 4380.0 | nM | 5.36 |
| CHEMBL97383 | — | Ki | = | 6960.0 | nM | 5.16 |