Assay Detail
Binding
CHEMBL649773
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Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| 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 | 12 | 6.15 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118164 | — | — | 1 | 8.44 |
| CHEMBL421420 | — | — | 1 | 7.12 |
| CHEMBL121593 | — | — | 1 | 7.10 |
| CHEMBL331946 | — | — | 1 | 6.74 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL16416 | — | — | 1 | 6.42 |
| CHEMBL116827 | — | — | 1 | 5.98 |
| CHEMBL334224 | — | — | 1 | 5.80 |
| CHEMBL332969 | — | — | 1 | 5.17 |
| CHEMBL121793 | — | — | 1 | 5.01 |
| CHEMBL120662 | — | — | 1 | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118164 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL421420 | — | Ki | = | 75.8 | nM | 7.12 |
| CHEMBL121593 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL331946 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL16416 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL116827 | — | Ki | = | 1049.0 | nM | 5.98 |
| CHEMBL334224 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL332969 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL121793 | — | Ki | = | 9700.0 | nM | 5.01 |
| CHEMBL120662 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 21000.0 | nM | 4.68 |