Assay Detail
Binding
CHEMBL1120796
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Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells
27
Total Activities
27
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
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.36 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.70 |
| CHEMBL1096410 | — | — | 1 | 7.02 |
| CHEMBL1094987 | — | — | 1 | 6.92 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.89 |
| CHEMBL1094143 | — | — | 1 | 6.74 |
| CHEMBL1098075 | — | — | 1 | 6.64 |
| CHEMBL1096409 | — | — | 1 | 6.50 |
| CHEMBL1096754 | — | — | 1 | 6.14 |
| CHEMBL1098109 | — | — | 1 | 6.05 |
| CHEMBL1097737 | — | — | 1 | 6.00 |
| CHEMBL1097050 | — | — | 1 | 5.95 |
| CHEMBL515442 | — | — | 1 | 5.68 |
| CHEMBL1098108 | — | — | 1 | 5.50 |
| CHEMBL1096693 | — | — | 1 | 5.31 |
| CHEMBL1096753 | — | — | 1 | - |
| CHEMBL1098445 | — | — | 1 | - |
| CHEMBL1098758 | — | — | 1 | - |
| CHEMBL1098759 | — | — | 1 | - |
| CHEMBL1099102 | — | — | 1 | - |
| CHEMBL1094131 | — | — | 1 | - |
| CHEMBL1094132 | — | — | 1 | - |
| CHEMBL1096078 | — | — | 1 | - |
| CHEMBL1097736 | — | — | 1 | - |
| CHEMBL1095747 | — | — | 1 | - |
| CHEMBL1095748 | — | — | 1 | - |
| CHEMBL1094442 | — | — | 1 | - |
| CHEMBL1096692 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1096410 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL1094987 | — | Ki | = | 121.1 | nM | 6.92 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL1094143 | — | Ki | = | 180.6 | nM | 6.74 |
| CHEMBL1098075 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL1096409 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL1096754 | — | Ki | = | 728.1 | nM | 6.14 |
| CHEMBL1098109 | — | Ki | = | 886.0 | nM | 6.05 |
| CHEMBL1097737 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1097050 | — | Ki | = | 1136.0 | nM | 5.95 |
| CHEMBL515442 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL1098108 | — | Ki | = | 3179.0 | nM | 5.50 |
| CHEMBL1096693 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL1096753 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1098445 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1098758 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1098759 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1099102 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1094131 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1094132 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1096078 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1097736 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1095747 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1095748 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1094442 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1096692 | — | Ki | > | 10000.0 | nM | - |