Assay Detail
Binding
CHEMBL640591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CGS- 21680 from rat striatal membranes Adenosine A2A receptor. Parenthesis indicate 95% confidence limits.
12
Total Activities
12
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
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.05 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL67026 | — | — | 1 | 9.03 |
| CHEMBL16687 | CGS-15943 | — | 1 | 9.02 |
| CHEMBL67994 | — | — | 1 | 8.77 |
| CHEMBL17127 | SCH-58261 | — | 1 | 8.64 |
| CHEMBL17121 | SCH-63390 | — | 1 | 8.62 |
| CHEMBL307748 | — | — | 1 | 8.42 |
| CHEMBL69794 | — | — | 1 | 8.28 |
| CHEMBL423852 | — | — | 1 | 7.35 |
| CHEMBL63520 | — | — | 1 | 7.31 |
| CHEMBL416684 | — | — | 1 | 7.28 |
| CHEMBL67134 | — | — | 1 | 7.23 |
| CHEMBL66811 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL67026 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL16687 | CGS-15943 | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL67994 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL17127 | SCH-58261 | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL17121 | SCH-63390 | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL307748 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL69794 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL423852 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL63520 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL416684 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL67134 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL66811 | — | Ki | = | 246.0 | nM | 6.61 |