Assay Detail
Binding
CHEMBL894344
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Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells
9
Total Activities
9
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 | 9 | 6.16 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL320805 | — | — | 1 | 7.04 |
| CHEMBL107446 | — | — | 1 | 6.64 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.58 |
| CHEMBL106346 | — | — | 1 | 6.48 |
| CHEMBL388458 | — | — | 1 | 6.31 |
| CHEMBL105913 | — | — | 1 | 5.97 |
| CHEMBL388459 | — | — | 1 | 5.82 |
| CHEMBL242424 | — | — | 1 | 5.54 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL320805 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL107446 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL106346 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL388458 | — | Ki | = | 486.0 | nM | 6.31 |
| CHEMBL105913 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL388459 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL242424 | — | Ki | = | 2860.0 | nM | 5.54 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 7900.0 | nM | 5.10 |