Assay Detail
Binding
CHEMBL894342
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
23
Total Activities
23
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 | 23 | 6.82 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.49 |
| CHEMBL387592 | — | — | 1 | 7.92 |
| CHEMBL388250 | — | — | 1 | 7.85 |
| CHEMBL107446 | — | — | 1 | 7.68 |
| CHEMBL242202 | — | — | 1 | 7.54 |
| CHEMBL388458 | — | — | 1 | 7.50 |
| CHEMBL105913 | — | — | 1 | 7.40 |
| CHEMBL106346 | — | — | 1 | 7.35 |
| CHEMBL242424 | — | — | 1 | 7.24 |
| CHEMBL242633 | — | — | 1 | 7.22 |
| CHEMBL242203 | — | — | 1 | 6.75 |
| CHEMBL390408 | — | — | 1 | 6.70 |
| CHEMBL242421 | — | — | 1 | 6.69 |
| CHEMBL241987 | — | — | 1 | 6.69 |
| CHEMBL390407 | — | — | 1 | 6.60 |
| CHEMBL242204 | — | — | 1 | 6.45 |
| CHEMBL388459 | — | — | 1 | 6.34 |
| CHEMBL242851 | — | — | 1 | 6.25 |
| CHEMBL242632 | — | — | 1 | 6.20 |
| CHEMBL320805 | — | — | 1 | 6.18 |
| CHEMBL242422 | — | — | 1 | 5.54 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.21 |
| CHEMBL231560 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL387592 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL388250 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL107446 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL242202 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL388458 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL105913 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL106346 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL242424 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL242633 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL242203 | — | Ki | = | 176.4 | nM | 6.75 |
| CHEMBL390408 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL242421 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL241987 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL390407 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL242204 | — | Ki | = | 357.0 | nM | 6.45 |
| CHEMBL388459 | — | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL242851 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL242632 | — | Ki | = | 629.0 | nM | 6.20 |
| CHEMBL320805 | — | Ki | = | 659.0 | nM | 6.18 |
| CHEMBL242422 | — | Ki | = | 2875.0 | nM | 5.54 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL231560 | — | Ki | = | 6800.0 | nM | 5.17 |