Assay Detail
Binding
CHEMBL643127
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Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 5.77 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119709 | IB-MECA | — | 1 | 8.96 |
| CHEMBL49843 | — | — | 1 | 7.80 |
| CHEMBL410873 | — | — | 1 | 7.59 |
| CHEMBL464859 | NECA | — | 1 | 6.95 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.92 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 6.44 |
| CHEMBL2113395 | — | — | 1 | 6.22 |
| CHEMBL2113396 | — | — | 1 | 6.15 |
| CHEMBL2113475 | — | — | 1 | 6.14 |
| CHEMBL411066 | KINETIN RIBOSIDE | — | 1 | 6.13 |
| CHEMBL2079643 | — | — | 1 | 5.96 |
| CHEMBL2113474 | — | — | 1 | 5.83 |
| CHEMBL285819 | — | — | 1 | 5.72 |
| CHEMBL2113392 | — | — | 1 | 5.61 |
| CHEMBL443485 | 5'-Deoxyadenosine | — | 1 | 5.55 |
| CHEMBL1568 | FLUDARABINE | 3.0 | 1 | 4.98 |
| CHEMBL471144 | — | — | 1 | 4.96 |
| CHEMBL236757 | — | — | 1 | 4.77 |
| CHEMBL17857 | — | — | 1 | 4.71 |
| CHEMBL2079570 | — | — | 1 | 4.31 |
| CHEMBL278932 | — | — | 1 | 4.23 |
| CHEMBL202701 | — | — | 1 | 4.21 |
| CHEMBL279158 | — | — | 1 | 4.15 |
| CHEMBL3142980 | — | — | 1 | 4.08 |
| CHEMBL1619 | CLADRIBINE | 4.0 | 1 | - |
| CHEMBL17875 | — | — | 1 | - |
| CHEMBL2112597 | — | — | 1 | - |
| CHEMBL416540 | — | — | 1 | - |
| CHEMBL49935 | ARISTEROMYCIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119709 | IB-MECA | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL49843 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL410873 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL464859 | NECA | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL2113395 | — | Ki | = | 604.0 | nM | 6.22 |
| CHEMBL2113396 | — | Ki | = | 703.0 | nM | 6.15 |
| CHEMBL2113475 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL411066 | KINETIN RIBOSIDE | Ki | = | 742.0 | nM | 6.13 |
| CHEMBL2079643 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL2113474 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL285819 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL2113392 | — | Ki | = | 2480.0 | nM | 5.61 |
| CHEMBL443485 | 5'-Deoxyadenosine | Ki | = | 2830.0 | nM | 5.55 |
| CHEMBL1568 | FLUDARABINE | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL471144 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL236757 | — | Ki | = | 16900.0 | nM | 4.77 |
| CHEMBL17857 | — | Ki | = | 19500.0 | nM | 4.71 |
| CHEMBL2079570 | — | Ki | = | 49300.0 | nM | 4.31 |
| CHEMBL278932 | — | Ki | = | 59200.0 | nM | 4.23 |
| CHEMBL202701 | — | Ki | = | 61700.0 | nM | 4.21 |
| CHEMBL279158 | — | Ki | = | 70400.0 | nM | 4.15 |
| CHEMBL3142980 | — | Ki | = | 82400.0 | nM | 4.08 |
| CHEMBL1619 | CLADRIBINE | Ki | = | 207000.0 | nM | - |
| CHEMBL17875 | — | Ki | = | 122000.0 | nM | - |
| CHEMBL2112597 | — | Ki | = | 199000.0 | nM | - |
| CHEMBL416540 | — | Ki | = | 198000.0 | nM | - |
| CHEMBL49935 | ARISTEROMYCIN | Ki | = | 200000.0 | nM | - |