Assay Detail
Binding
CHEMBL1012742
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGS 21680 from bovine striatal membrane adenosine A2A receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 10 | 6.10 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL474636 | — | — | 1 | 7.03 |
| CHEMBL473648 | — | — | 1 | 6.70 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL474977 | — | — | 1 | 6.38 |
| CHEMBL473839 | — | — | 1 | 6.38 |
| CHEMBL473649 | — | — | 1 | 6.29 |
| CHEMBL514155 | — | — | 1 | 6.08 |
| CHEMBL515433 | — | — | 1 | 5.82 |
| CHEMBL473650 | — | — | 1 | 5.15 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL474636 | — | Ki | = | 92.6 | nM | 7.03 |
| CHEMBL473648 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL474977 | — | Ki | = | 413.0 | nM | 6.38 |
| CHEMBL473839 | — | Ki | = | 414.0 | nM | 6.38 |
| CHEMBL473649 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL514155 | — | Ki | = | 832.0 | nM | 6.08 |
| CHEMBL515433 | — | Ki | = | 1508.0 | nM | 5.82 |
| CHEMBL473650 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 21000.0 | nM | 4.68 |