Assay Detail
Functional
CHEMBL2073181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
32
Total Activities
32
Compounds Tested
2
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 | 5.77 | 6.30 |
| Ki | 2 | 6.14 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118923 | — | — | 1 | 6.60 |
| CHEMBL2071047 | — | — | 1 | 6.30 |
| CHEMBL2071046 | — | — | 1 | 5.98 |
| CHEMBL2071044 | — | — | 1 | 5.96 |
| CHEMBL2071045 | — | — | 1 | 5.81 |
| CHEMBL2069325 | — | — | 1 | 5.76 |
| CHEMBL2070886 | — | — | 1 | 5.69 |
| CHEMBL302765 | — | — | 1 | 5.68 |
| CHEMBL2071051 | — | — | 1 | 5.67 |
| CHEMBL2071048 | — | — | 1 | 5.67 |
| CHEMBL2070880 | — | — | 1 | 5.62 |
| CHEMBL2071050 | — | — | 1 | 5.49 |
| CHEMBL2071049 | — | — | 1 | 5.49 |
| CHEMBL2070883 | — | — | 1 | - |
| CHEMBL2070884 | — | — | 1 | - |
| CHEMBL2070885 | — | — | 1 | - |
| CHEMBL2070887 | — | — | 1 | - |
| CHEMBL2070888 | — | — | 1 | - |
| CHEMBL2070889 | — | — | 1 | - |
| CHEMBL2070890 | — | — | 1 | - |
| CHEMBL2070891 | — | — | 1 | - |
| CHEMBL2070892 | — | — | 1 | - |
| CHEMBL2070893 | — | — | 1 | - |
| CHEMBL2070894 | — | — | 1 | - |
| CHEMBL2071038 | — | — | 1 | - |
| CHEMBL2071040 | — | — | 1 | - |
| CHEMBL2071041 | — | — | 1 | - |
| CHEMBL2071042 | — | — | 1 | - |
| CHEMBL2071043 | — | — | 1 | - |
| CHEMBL2071039 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118923 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2071047 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL2071046 | — | IC50 | = | 1042.0 | nM | 5.98 |
| CHEMBL2071044 | — | IC50 | = | 1107.0 | nM | 5.96 |
| CHEMBL2071045 | — | IC50 | = | 1542.0 | nM | 5.81 |
| CHEMBL2069325 | — | IC50 | = | 1755.0 | nM | 5.76 |
| CHEMBL2070886 | — | IC50 | = | 2061.0 | nM | 5.69 |
| CHEMBL302765 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL2071051 | — | IC50 | = | 2144.0 | nM | 5.67 |
| CHEMBL2071048 | — | IC50 | = | 2122.0 | nM | 5.67 |
| CHEMBL2070880 | — | IC50 | = | 2428.0 | nM | 5.62 |
| CHEMBL2071050 | — | IC50 | = | 3235.0 | nM | 5.49 |
| CHEMBL2071049 | — | IC50 | = | 3244.0 | nM | 5.49 |
| CHEMBL2070881 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070882 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070883 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070884 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070885 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070887 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070888 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070889 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070890 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070891 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070892 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070893 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2070894 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2071038 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2071040 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2071041 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2071042 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2071043 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2071039 | — | IC50 | > | 5000.0 | nM | - |