Assay Detail
Binding
CHEMBL860157
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Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells
29
Total Activities
29
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 | 29 | 7.02 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328437 | — | — | 1 | 8.70 |
| CHEMBL99178 | — | — | 1 | 8.68 |
| CHEMBL197376 | — | — | 1 | 8.60 |
| CHEMBL200479 | — | — | 1 | 8.54 |
| CHEMBL316824 | — | — | 1 | 8.22 |
| CHEMBL110165 | — | — | 1 | 7.60 |
| CHEMBL98678 | — | — | 1 | 7.59 |
| CHEMBL178863 | — | — | 1 | 7.55 |
| CHEMBL330399 | — | — | 1 | 7.48 |
| CHEMBL325715 | — | — | 1 | 7.29 |
| CHEMBL86164 | — | — | 1 | 7.15 |
| CHEMBL327853 | — | — | 1 | 7.11 |
| CHEMBL334286 | — | — | 1 | 7.09 |
| CHEMBL200835 | — | — | 1 | 7.04 |
| CHEMBL9128 | — | — | 1 | 6.97 |
| CHEMBL197325 | — | — | 1 | 6.96 |
| CHEMBL97286 | — | — | 1 | 6.90 |
| CHEMBL198574 | — | — | 1 | 6.79 |
| CHEMBL94830 | — | — | 1 | 6.59 |
| CHEMBL371697 | — | — | 1 | 6.51 |
| CHEMBL83919 | — | — | 1 | 6.47 |
| CHEMBL310544 | — | — | 1 | 6.45 |
| CHEMBL197333 | — | — | 1 | 6.40 |
| CHEMBL116737 | — | — | 1 | 6.38 |
| CHEMBL83855 | — | — | 1 | 6.25 |
| CHEMBL8907 | — | — | 1 | 6.17 |
| CHEMBL179109 | — | — | 1 | 6.09 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 5.89 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328437 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL99178 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL197376 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL200479 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL316824 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL110165 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL98678 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL178863 | — | Ki | = | 28.2 | nM | 7.55 |
| CHEMBL330399 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL325715 | — | Ki | = | 51.6 | nM | 7.29 |
| CHEMBL86164 | — | Ki | = | 70.8 | nM | 7.15 |
| CHEMBL327853 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL334286 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL200835 | — | Ki | = | 91.4 | nM | 7.04 |
| CHEMBL9128 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL197325 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL97286 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL198574 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL94830 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL371697 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL83919 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL310544 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL197333 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL116737 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL83855 | — | Ki | = | 557.0 | nM | 6.25 |
| CHEMBL8907 | — | Ki | = | 673.0 | nM | 6.17 |
| CHEMBL179109 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 86000.0 | nM | 4.07 |