Assay Detail
Binding
CHEMBL862970
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells
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
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 | 7 | 6.68 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.49 |
| CHEMBL209927 | — | — | 1 | 7.73 |
| CHEMBL16488 | — | — | 1 | 7.06 |
| CHEMBL211183 | — | — | 1 | 7.01 |
| CHEMBL16305 | — | — | 1 | 5.70 |
| CHEMBL210642 | — | — | 1 | 5.57 |
| 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 |
| CHEMBL209927 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL16488 | — | Ki | = | 87.8 | nM | 7.06 |
| CHEMBL211183 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL16305 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL210642 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6200.0 | nM | 5.21 |