Assay Detail
Binding
CHEMBL1936134
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Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 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 | 7.08 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1935745 | — | — | 1 | 8.37 |
| CHEMBL1935762 | — | — | 1 | 8.31 |
| CHEMBL1935763 | — | — | 1 | 8.15 |
| CHEMBL1935752 | — | — | 1 | 8.00 |
| CHEMBL1935768 | — | — | 1 | 7.92 |
| CHEMBL1935753 | — | — | 1 | 7.85 |
| CHEMBL1935746 | — | — | 1 | 7.75 |
| CHEMBL1935761 | — | — | 1 | 7.66 |
| CHEMBL1935760 | — | — | 1 | 7.52 |
| CHEMBL1935754 | — | — | 1 | 7.48 |
| CHEMBL1935744 | — | — | 1 | 7.46 |
| CHEMBL1935757 | — | — | 1 | 7.21 |
| CHEMBL1935755 | — | — | 1 | 7.07 |
| CHEMBL1935743 | — | — | 1 | 7.00 |
| CHEMBL1935756 | — | — | 1 | 6.89 |
| CHEMBL1935749 | — | — | 1 | 6.75 |
| CHEMBL1935750 | — | — | 1 | 6.68 |
| CHEMBL1935765 | — | — | 1 | 6.62 |
| CHEMBL332091 | — | — | 1 | 6.60 |
| CHEMBL17121 | SCH-63390 | — | 1 | 6.46 |
| CHEMBL1935751 | — | — | 1 | 6.45 |
| CHEMBL1935758 | — | — | 1 | 6.28 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.26 |
| CHEMBL1935748 | — | — | 1 | 6.13 |
| CHEMBL1935766 | — | — | 1 | 6.12 |
| CHEMBL1935747 | — | — | 1 | 6.10 |
| CHEMBL1935764 | — | — | 1 | 6.04 |
| CHEMBL1935759 | — | — | 1 | - |
| CHEMBL1935767 | — | — | 1 | - |
| CHEMBL1935769 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1935745 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL1935762 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL1935763 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL1935752 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1935768 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1935753 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1935746 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1935761 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1935760 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1935754 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL1935744 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1935757 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1935755 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL1935743 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1935756 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL1935749 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL1935750 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL1935765 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL332091 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL17121 | SCH-63390 | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL1935751 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL1935758 | — | Ki | = | 524.0 | nM | 6.28 |
| CHEMBL17127 | SCH-58261 | Ki | = | 549.0 | nM | 6.26 |
| CHEMBL1935748 | — | Ki | = | 743.0 | nM | 6.13 |
| CHEMBL1935766 | — | Ki | = | 753.0 | nM | 6.12 |
| CHEMBL1935747 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL1935764 | — | Ki | = | 923.0 | nM | 6.04 |
| 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 | - |