Assay Detail
Binding
CHEMBL860040
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CHA from cloned human adenosine A1 receptor expressed in CHO cells
10
Total Activities
10
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[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.17 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328437 | — | — | 1 | 8.70 |
| CHEMBL197376 | — | — | 1 | 8.54 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.49 |
| CHEMBL98678 | — | — | 1 | 8.48 |
| CHEMBL200479 | — | — | 1 | 7.44 |
| CHEMBL327853 | — | — | 1 | 6.90 |
| CHEMBL334286 | — | — | 1 | 6.69 |
| CHEMBL330399 | — | — | 1 | 5.71 |
| CHEMBL316824 | — | — | 1 | 5.56 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328437 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL197376 | — | Ki | = | 2.86 | nM | 8.54 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL98678 | — | Ki | = | 3.29 | nM | 8.48 |
| CHEMBL200479 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL327853 | — | Ki | = | 124.7 | nM | 6.90 |
| CHEMBL334286 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL330399 | — | Ki | = | 1926.0 | nM | 5.71 |
| CHEMBL316824 | — | Ki | = | 2740.0 | nM | 5.56 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6200.0 | nM | 5.21 |