Assay Detail
Binding
CHEMBL1012734
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells
27
Total Activities
27
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 | Autocuration |
Publication
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop 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 | 27 | 7.01 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475791 | — | — | 1 | 8.48 |
| CHEMBL474016 | — | — | 1 | 8.34 |
| CHEMBL333799 | — | — | 1 | 8.33 |
| CHEMBL421420 | — | — | 1 | 8.32 |
| CHEMBL475026 | — | — | 1 | 8.11 |
| CHEMBL473649 | — | — | 1 | 8.08 |
| CHEMBL473839 | — | — | 1 | 7.93 |
| CHEMBL473648 | — | — | 1 | 7.81 |
| CHEMBL378276 | — | — | 1 | 7.66 |
| CHEMBL516049 | — | — | 1 | 7.39 |
| CHEMBL120714 | — | — | 1 | 7.33 |
| CHEMBL473650 | — | — | 1 | 7.15 |
| CHEMBL492955 | — | — | 1 | 6.94 |
| CHEMBL514156 | — | — | 1 | 6.86 |
| CHEMBL474977 | — | — | 1 | 6.80 |
| CHEMBL212639 | — | — | 1 | 6.66 |
| CHEMBL514196 | — | — | 1 | 6.60 |
| CHEMBL508031 | — | — | 1 | 6.55 |
| CHEMBL492356 | — | — | 1 | 6.55 |
| CHEMBL516372 | — | — | 1 | 6.47 |
| CHEMBL377781 | — | — | 1 | 6.47 |
| CHEMBL515433 | — | — | 1 | 6.31 |
| CHEMBL475792 | — | — | 1 | 6.23 |
| CHEMBL474636 | — | — | 1 | 6.18 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 5.89 |
| CHEMBL514155 | — | — | 1 | 5.88 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475791 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL474016 | — | Ki | = | 4.54 | nM | 8.34 |
| CHEMBL333799 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL421420 | — | Ki | = | 4.75 | nM | 8.32 |
| CHEMBL475026 | — | Ki | = | 7.75 | nM | 8.11 |
| CHEMBL473649 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL473839 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL473648 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL378276 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL516049 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL120714 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL473650 | — | Ki | = | 70.3 | nM | 7.15 |
| CHEMBL492955 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL514156 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL474977 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL212639 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL514196 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL508031 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL492356 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL516372 | — | Ki | = | 335.0 | nM | 6.47 |
| CHEMBL377781 | — | Ki | = | 342.0 | nM | 6.47 |
| CHEMBL515433 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL475792 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL474636 | — | Ki | = | 656.0 | nM | 6.18 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL514155 | — | Ki | = | 1335.0 | nM | 5.88 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 86000.0 | nM | 4.07 |