Assay Detail
Binding
CHEMBL955679
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Displacement of [3H]CGS21680 from adenosine A2A receptor in bovine brain membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.03 | 6.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL508203 | — | — | 1 | 6.76 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL484314 | — | — | 1 | 6.42 |
| CHEMBL502005 | — | — | 1 | 6.09 |
| CHEMBL484520 | — | — | 1 | 5.75 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL508203 | — | Ki | = | 172.6 | nM | 6.76 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL484314 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL502005 | — | Ki | = | 812.0 | nM | 6.09 |
| CHEMBL484520 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 21000.0 | nM | 4.68 |