Assay Detail
Binding
CHEMBL864191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes
5
Total Activities
5
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
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 5.49 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL209927 | — | — | 1 | 5.94 |
| CHEMBL378514 | — | — | 1 | 5.20 |
| CHEMBL212458 | — | — | 1 | 5.18 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL209927 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL378514 | — | Ki | = | 6250.0 | nM | 5.20 |
| CHEMBL212458 | — | Ki | = | 6570.0 | nM | 5.18 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 21000.0 | nM | 4.68 |