Assay Detail
Binding
CHEMBL638723
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Binding affinity against adenosine A1 receptor in bovine brain membranes by [3H]CHA displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| 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 | 18 | 6.82 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL118679 | — | — | 1 | 8.06 |
| CHEMBL121793 | — | — | 1 | 7.58 |
| CHEMBL332969 | — | — | 1 | 7.51 |
| CHEMBL118164 | — | — | 1 | 7.32 |
| CHEMBL331946 | — | — | 1 | 7.21 |
| CHEMBL421420 | — | — | 1 | 7.09 |
| CHEMBL120346 | — | — | 1 | 7.04 |
| CHEMBL121593 | — | — | 1 | 6.94 |
| CHEMBL331540 | — | — | 1 | 6.81 |
| CHEMBL16416 | — | — | 1 | 6.51 |
| CHEMBL334224 | — | — | 1 | 6.35 |
| CHEMBL120662 | — | — | 1 | 6.27 |
| CHEMBL333943 | — | — | 1 | 6.24 |
| CHEMBL16737 | — | — | 1 | 6.03 |
| CHEMBL333872 | — | — | 1 | 6.00 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.42 |
| CHEMBL120602 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL118679 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL121793 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL332969 | — | Ki | = | 30.6 | nM | 7.51 |
| CHEMBL118164 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL331946 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL421420 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL120346 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL121593 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL331540 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL16416 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL334224 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL120662 | — | Ki | = | 537.0 | nM | 6.27 |
| CHEMBL333943 | — | Ki | = | 577.7 | nM | 6.24 |
| CHEMBL16737 | — | Ki | = | 934.0 | nM | 6.03 |
| CHEMBL333872 | — | Ki | = | 996.0 | nM | 6.00 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL120602 | — | Ki | = | 10000.0 | nM | 5.00 |