Assay Detail
Binding
CHEMBL894340
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Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells
25
Total Activities
25
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
New 2-arylpyrazolo[3,4-c]quinoline derivatives as 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 | 25 | 7.55 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL231560 | — | — | 1 | 8.47 |
| CHEMBL390407 | — | — | 1 | 8.47 |
| CHEMBL242633 | — | — | 1 | 8.41 |
| CHEMBL242424 | — | — | 1 | 8.37 |
| CHEMBL242632 | — | — | 1 | 8.36 |
| CHEMBL390408 | — | — | 1 | 8.35 |
| CHEMBL242634 | — | — | 1 | 8.25 |
| CHEMBL389318 | — | — | 1 | 8.21 |
| CHEMBL388250 | — | — | 1 | 8.14 |
| CHEMBL242849 | — | — | 1 | 8.05 |
| CHEMBL397033 | — | — | 1 | 8.05 |
| CHEMBL388947 | — | — | 1 | 7.94 |
| CHEMBL242851 | — | — | 1 | 7.85 |
| CHEMBL230854 | — | — | 1 | 7.76 |
| CHEMBL230853 | — | — | 1 | 7.63 |
| CHEMBL389962 | — | — | 1 | 7.52 |
| CHEMBL242421 | — | — | 1 | 7.51 |
| CHEMBL242205 | — | — | 1 | 7.13 |
| CHEMBL242204 | — | — | 1 | 7.07 |
| CHEMBL242422 | — | — | 1 | 6.99 |
| CHEMBL388459 | — | — | 1 | 6.91 |
| CHEMBL388458 | — | — | 1 | 6.64 |
| CHEMBL425671 | — | — | 1 | 6.59 |
| 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 |
|---|---|---|---|---|---|---|
| CHEMBL231560 | — | Ki | = | 3.35 | nM | 8.47 |
| CHEMBL390407 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL242633 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL242424 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL242632 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL390408 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL242634 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL389318 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL388250 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL242849 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL397033 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL388947 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL242851 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL230854 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL230853 | — | Ki | = | 23.25 | nM | 7.63 |
| CHEMBL389962 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL242421 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL242205 | — | Ki | = | 74.5 | nM | 7.13 |
| CHEMBL242204 | — | Ki | = | 85.5 | nM | 7.07 |
| CHEMBL242422 | — | Ki | = | 101.5 | nM | 6.99 |
| CHEMBL388459 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL388458 | — | Ki | = | 228.5 | nM | 6.64 |
| CHEMBL425671 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 86000.0 | nM | 4.07 |