Assay Detail
Binding
CHEMBL1012738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NECA from human cloned adenosine A2A receptor expressed in CHO cells
6
Total Activities
6
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 | 6 | 6.23 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473648 | — | — | 1 | 6.68 |
| CHEMBL473649 | — | — | 1 | 6.68 |
| CHEMBL473839 | — | — | 1 | 6.68 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.58 |
| CHEMBL473650 | — | — | 1 | 5.65 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473648 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL473649 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL473839 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL473650 | — | Ki | = | 2240.0 | nM | 5.65 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 7900.0 | nM | 5.10 |