Assay Detail
Binding
CHEMBL1120797
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Displacement of [125I]AB-MECA from human adenosine A3 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 | 7.65 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1098108 | — | — | 1 | 9.74 |
| CHEMBL1096754 | — | — | 1 | 9.22 |
| CHEMBL1096078 | — | — | 1 | 8.54 |
| CHEMBL1094132 | — | — | 1 | 8.54 |
| CHEMBL1094143 | — | — | 1 | 8.52 |
| CHEMBL1094131 | — | — | 1 | 8.43 |
| CHEMBL1098109 | — | — | 1 | 8.23 |
| CHEMBL464859 | NECA | — | 1 | 8.21 |
| CHEMBL515442 | — | — | 1 | 7.96 |
| CHEMBL1098445 | — | — | 1 | 7.68 |
| CHEMBL1099102 | — | — | 1 | 7.66 |
| CHEMBL1096409 | — | — | 1 | 7.65 |
| CHEMBL1098759 | — | — | 1 | 7.54 |
| CHEMBL1096410 | — | — | 1 | 7.44 |
| CHEMBL1098075 | — | — | 1 | 7.36 |
| CHEMBL1097050 | — | — | 1 | 7.34 |
| CHEMBL1094987 | — | — | 1 | 7.03 |
| CHEMBL1097736 | — | — | 1 | 6.92 |
| CHEMBL1098758 | — | — | 1 | 6.45 |
| CHEMBL1097737 | — | — | 1 | 6.30 |
| CHEMBL1096753 | — | — | 1 | 6.04 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 5.40 |
| CHEMBL1095747 | — | — | 1 | - |
| CHEMBL1095748 | — | — | 1 | - |
| CHEMBL1094442 | — | — | 1 | - |
| CHEMBL1096692 | — | — | 1 | - |
| CHEMBL1096693 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1098108 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1096754 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1096078 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1094132 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1094143 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1094131 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1098109 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL464859 | NECA | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL515442 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1098445 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL1099102 | — | Ki | = | 22.1 | nM | 7.66 |
| CHEMBL1096409 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL1098759 | — | Ki | = | 29.1 | nM | 7.54 |
| CHEMBL1096410 | — | Ki | = | 36.3 | nM | 7.44 |
| CHEMBL1098075 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL1097050 | — | Ki | = | 45.2 | nM | 7.34 |
| CHEMBL1094987 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL1097736 | — | Ki | = | 120.8 | nM | 6.92 |
| CHEMBL1098758 | — | Ki | = | 357.9 | nM | 6.45 |
| CHEMBL1097737 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL1096753 | — | Ki | = | 922.0 | nM | 6.04 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL1095747 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1095748 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094442 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1096692 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1096693 | — | Ki | > | 1000.0 | nM | - |