Assay Detail
Binding
CHEMBL955671
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Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells
20
Total Activities
20
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
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.96 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16488 | — | — | 1 | 8.83 |
| CHEMBL482701 | — | — | 1 | 8.66 |
| CHEMBL519319 | — | — | 1 | 8.26 |
| CHEMBL502005 | — | — | 1 | 8.21 |
| CHEMBL484721 | — | — | 1 | 8.19 |
| CHEMBL484720 | — | — | 1 | 7.68 |
| CHEMBL482504 | — | — | 1 | 7.49 |
| CHEMBL484313 | — | — | 1 | 7.20 |
| CHEMBL484112 | — | — | 1 | 7.19 |
| CHEMBL526134 | — | — | 1 | 7.17 |
| CHEMBL508203 | — | — | 1 | 7.08 |
| CHEMBL483309 | — | — | 1 | 7.00 |
| CHEMBL520152 | — | — | 1 | 6.41 |
| CHEMBL483115 | — | — | 1 | 6.31 |
| CHEMBL484520 | — | — | 1 | 6.02 |
| CHEMBL484314 | — | — | 1 | 5.89 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 5.89 |
| CHEMBL484299 | — | — | 1 | 5.86 |
| CHEMBL483310 | — | — | 1 | 5.85 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16488 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL482701 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL519319 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL502005 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL484721 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL484720 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL482504 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL484313 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL484112 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL526134 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL508203 | — | Ki | = | 83.5 | nM | 7.08 |
| CHEMBL483309 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL520152 | — | Ki | = | 387.0 | nM | 6.41 |
| CHEMBL483115 | — | Ki | = | 493.0 | nM | 6.31 |
| CHEMBL484520 | — | Ki | = | 953.0 | nM | 6.02 |
| CHEMBL484314 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL484299 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL483310 | — | Ki | = | 1427.0 | nM | 5.85 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 86000.0 | nM | 4.07 |