Assay Detail
Binding
CHEMBL861067
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Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.58 | 6.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200835 | — | — | 1 | 6.79 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL330399 | — | — | 1 | 5.32 |
| CHEMBL8966 | — | — | 1 | 5.31 |
| CHEMBL316824 | — | — | 1 | 5.29 |
| CHEMBL94830 | — | — | 1 | 5.18 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200835 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL330399 | — | Ki | = | 4750.0 | nM | 5.32 |
| CHEMBL8966 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL316824 | — | Ki | = | 5160.0 | nM | 5.29 |
| CHEMBL94830 | — | Ki | = | 6530.0 | nM | 5.18 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 21000.0 | nM | 4.68 |