Assay Detail
Binding
CHEMBL955675
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]NECA from human cloned adenosine A2A receptor expressed in CHO cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| 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 | 6.44 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16488 | — | — | 1 | 7.05 |
| CHEMBL508203 | — | — | 1 | 6.80 |
| CHEMBL502005 | — | — | 1 | 6.73 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.58 |
| CHEMBL526134 | — | — | 1 | 6.40 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16488 | — | Ki | = | 88.2 | nM | 7.05 |
| CHEMBL508203 | — | Ki | = | 158.3 | nM | 6.80 |
| CHEMBL502005 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL526134 | — | Ki | = | 397.0 | nM | 6.40 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 7900.0 | nM | 5.10 |