Assay Detail
Binding
CHEMBL955673
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Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells
8
Total Activities
8
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 | 8 | 6.42 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.49 |
| CHEMBL508203 | — | — | 1 | 7.91 |
| CHEMBL16488 | — | — | 1 | 7.06 |
| CHEMBL526134 | — | — | 1 | 6.11 |
| CHEMBL502005 | — | — | 1 | 5.62 |
| CHEMBL482701 | — | — | 1 | 5.57 |
| CHEMBL484112 | — | — | 1 | 5.38 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL508203 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL16488 | — | Ki | = | 87.8 | nM | 7.06 |
| CHEMBL526134 | — | Ki | = | 779.0 | nM | 6.11 |
| CHEMBL502005 | — | Ki | = | 2379.0 | nM | 5.62 |
| CHEMBL482701 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL484112 | — | Ki | = | 4215.0 | nM | 5.38 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6200.0 | nM | 5.21 |