Assay Detail
Functional
CHEMBL2073225
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Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.18 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2071048 | — | — | 1 | 7.92 |
| CHEMBL2071046 | — | — | 1 | 7.82 |
| CHEMBL2069325 | — | — | 1 | 7.64 |
| CHEMBL2071043 | — | — | 1 | 7.58 |
| CHEMBL2071044 | — | — | 1 | 7.54 |
| CHEMBL2070885 | — | — | 1 | 7.52 |
| CHEMBL2071041 | — | — | 1 | 7.52 |
| CHEMBL2071049 | — | — | 1 | 7.47 |
| CHEMBL2071040 | — | — | 1 | 7.47 |
| CHEMBL2070891 | — | — | 1 | 7.40 |
| CHEMBL2071038 | — | — | 1 | 7.39 |
| CHEMBL2070892 | — | — | 1 | 7.38 |
| CHEMBL2071042 | — | — | 1 | 7.36 |
| CHEMBL2070890 | — | — | 1 | 7.35 |
| CHEMBL2071045 | — | — | 1 | 7.34 |
| CHEMBL2070889 | — | — | 1 | 7.30 |
| CHEMBL2070887 | — | — | 1 | 7.09 |
| CHEMBL2071050 | — | — | 1 | 7.09 |
| CHEMBL2071047 | — | — | 1 | 7.05 |
| CHEMBL2070888 | — | — | 1 | 7.04 |
| CHEMBL2070884 | — | — | 1 | 6.98 |
| CHEMBL2071039 | — | — | 1 | 6.94 |
| CHEMBL2071051 | — | — | 1 | 6.92 |
| CHEMBL2070886 | — | — | 1 | 6.92 |
| CHEMBL2070894 | — | — | 1 | 6.78 |
| CHEMBL2070893 | — | — | 1 | 6.75 |
| CHEMBL2070883 | — | — | 1 | 6.67 |
| CHEMBL2070880 | — | — | 1 | 6.58 |
| CHEMBL2070882 | — | — | 1 | 6.52 |
| CHEMBL2070881 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2071048 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2071046 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2069325 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2071043 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2071044 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2070885 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2071041 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2071049 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2071040 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2070891 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2071038 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2070892 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2071042 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2070890 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2071045 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2070889 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2070887 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2071050 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2071047 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2070888 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2070884 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL2071039 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL2071051 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2070886 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL2070894 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL2070893 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2070883 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL2070880 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL2070882 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL2070881 | — | IC50 | = | 910.0 | nM | 6.04 |