Assay Detail
Binding
CHEMBL1936135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ZM 241385 from human adenosine A2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting
32
Total Activities
32
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
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 7.41 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17127 | SCH-58261 | — | 1 | 8.96 |
| CHEMBL17121 | SCH-63390 | — | 1 | 8.92 |
| CHEMBL1935752 | — | — | 1 | 8.44 |
| CHEMBL1935745 | — | — | 1 | 8.41 |
| CHEMBL1935760 | — | — | 1 | 8.09 |
| CHEMBL1935762 | — | — | 1 | 8.04 |
| CHEMBL1935763 | — | — | 1 | 7.96 |
| CHEMBL1935753 | — | — | 1 | 7.92 |
| CHEMBL1935761 | — | — | 1 | 7.77 |
| CHEMBL1935743 | — | — | 1 | 7.70 |
| CHEMBL1935757 | — | — | 1 | 7.70 |
| CHEMBL1935744 | — | — | 1 | 7.52 |
| CHEMBL1935754 | — | — | 1 | 7.38 |
| CHEMBL1935746 | — | — | 1 | 7.30 |
| CHEMBL332091 | — | — | 1 | 7.22 |
| CHEMBL1935756 | — | — | 1 | 7.17 |
| CHEMBL1935768 | — | — | 1 | 6.92 |
| CHEMBL1935755 | — | — | 1 | 6.91 |
| CHEMBL1935750 | — | — | 1 | 6.89 |
| CHEMBL1935749 | — | — | 1 | 6.83 |
| CHEMBL1935748 | — | — | 1 | 6.70 |
| CHEMBL1935765 | — | — | 1 | 6.68 |
| CHEMBL1935764 | — | — | 1 | 6.65 |
| CHEMBL1935747 | — | — | 1 | 6.30 |
| CHEMBL1935758 | — | — | 1 | 6.20 |
| CHEMBL1935766 | — | — | 1 | 6.17 |
| CHEMBL1935751 | — | — | 1 | - |
| CHEMBL1935759 | — | — | 1 | - |
| CHEMBL1935767 | — | — | 1 | - |
| CHEMBL1935769 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17127 | SCH-58261 | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL17121 | SCH-63390 | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1935752 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1935745 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1935760 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL1935762 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL1935763 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1935753 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1935761 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1935743 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1935757 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1935744 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1935754 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1935746 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL332091 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL1935756 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1935768 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL1935755 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1935750 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL1935749 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL1935748 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1935765 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL1935764 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL1935747 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL1935758 | — | Ki | = | 626.0 | nM | 6.20 |
| CHEMBL1935766 | — | Ki | = | 672.0 | nM | 6.17 |
| CHEMBL1935751 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1935759 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1935767 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1935769 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1935770 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1935771 | — | Ki | > | 1000.0 | nM | - |