Assay Detail
Binding
CHEMBL643495
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Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]CHA
7
Total Activities
7
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 | Expert |
Publication
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.70 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.49 |
| CHEMBL16416 | — | — | 1 | 7.16 |
| CHEMBL332969 | — | — | 1 | 6.78 |
| CHEMBL116827 | — | — | 1 | 6.73 |
| CHEMBL121793 | — | — | 1 | 6.50 |
| CHEMBL421420 | — | — | 1 | 6.06 |
| 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 |
| CHEMBL16416 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL332969 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL116827 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL121793 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL421420 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6200.0 | nM | 5.21 |