Assay Detail
Binding
CHEMBL641303
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Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes.
19
Total Activities
19
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
Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.23 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL162666 | — | — | 1 | 7.99 |
| CHEMBL163626 | — | — | 1 | 7.58 |
| CHEMBL349191 | — | — | 1 | 5.94 |
| CHEMBL111545 | — | — | 1 | 5.69 |
| CHEMBL350988 | — | — | 1 | 5.25 |
| CHEMBL2112931 | — | — | 1 | 5.21 |
| CHEMBL321845 | — | — | 1 | 5.21 |
| CHEMBL164321 | — | — | 1 | 5.13 |
| CHEMBL159631 | — | — | 1 | 5.06 |
| CHEMBL163126 | — | — | 1 | 5.06 |
| CHEMBL422184 | — | — | 1 | 5.01 |
| CHEMBL164200 | — | — | 1 | 4.85 |
| CHEMBL163743 | — | — | 1 | 4.61 |
| CHEMBL164210 | — | — | 1 | 4.56 |
| CHEMBL164302 | — | — | 1 | 4.55 |
| CHEMBL352083 | — | — | 1 | 4.54 |
| CHEMBL347423 | — | — | 1 | 4.51 |
| CHEMBL163488 | — | — | 1 | 4.36 |
| CHEMBL348766 | — | — | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL162666 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL163626 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL349191 | — | Ki | = | 1140.0 | nM | 5.94 |
| CHEMBL111545 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL350988 | — | Ki | = | 5590.0 | nM | 5.25 |
| CHEMBL2112931 | — | Ki | = | 6140.0 | nM | 5.21 |
| CHEMBL321845 | — | Ki | = | 6130.0 | nM | 5.21 |
| CHEMBL164321 | — | Ki | = | 7330.0 | nM | 5.13 |
| CHEMBL159631 | — | Ki | = | 8760.0 | nM | 5.06 |
| CHEMBL163126 | — | Ki | = | 8630.0 | nM | 5.06 |
| CHEMBL422184 | — | Ki | = | 9670.0 | nM | 5.01 |
| CHEMBL164200 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL163743 | — | Ki | = | 24800.0 | nM | 4.61 |
| CHEMBL164210 | — | Ki | = | 27400.0 | nM | 4.56 |
| CHEMBL164302 | — | Ki | = | 28100.0 | nM | 4.55 |
| CHEMBL352083 | — | Ki | = | 29100.0 | nM | 4.54 |
| CHEMBL347423 | — | Ki | = | 30800.0 | nM | 4.51 |
| CHEMBL163488 | — | Ki | = | 43600.0 | nM | 4.36 |
| CHEMBL348766 | — | Ki | = | 67100.0 | nM | 4.17 |