Assay Detail
Binding
CHEMBL644951
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Binding affinity against human adenosine A3 receptor expressed in CHO cells by [125I]AB-MECA displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.05 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324095 | — | — | 1 | 9.22 |
| CHEMBL333799 | — | — | 1 | 8.33 |
| CHEMBL421420 | — | — | 1 | 8.32 |
| CHEMBL121793 | — | — | 1 | 7.95 |
| CHEMBL16737 | — | — | 1 | 7.80 |
| CHEMBL116827 | — | — | 1 | 7.66 |
| CHEMBL16416 | — | — | 1 | 7.35 |
| CHEMBL120714 | — | — | 1 | 7.33 |
| CHEMBL332969 | — | — | 1 | 7.33 |
| CHEMBL121593 | — | — | 1 | 7.13 |
| CHEMBL333016 | — | — | 1 | 7.08 |
| CHEMBL120602 | — | — | 1 | 6.76 |
| CHEMBL331946 | — | — | 1 | 6.75 |
| CHEMBL120662 | — | — | 1 | 6.69 |
| CHEMBL118164 | — | — | 1 | 6.47 |
| CHEMBL333943 | — | — | 1 | 6.37 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 5.89 |
| CHEMBL118679 | — | — | 1 | 5.44 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324095 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL333799 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL421420 | — | Ki | = | 4.75 | nM | 8.32 |
| CHEMBL121793 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL16737 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL116827 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL16416 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL120714 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL332969 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL121593 | — | Ki | = | 73.2 | nM | 7.13 |
| CHEMBL333016 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL120602 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL331946 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL120662 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL118164 | — | Ki | = | 335.0 | nM | 6.47 |
| CHEMBL333943 | — | Ki | = | 429.0 | nM | 6.37 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL118679 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 86000.0 | nM | 4.07 |