Assay Detail
Binding
CHEMBL647731
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| 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 | 34 | 5.86 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL410873 | — | — | 1 | 8.66 |
| CHEMBL464859 | NECA | — | 1 | 7.99 |
| CHEMBL2079643 | — | — | 1 | 7.70 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 7.62 |
| CHEMBL1568 | FLUDARABINE | 3.0 | 1 | 7.55 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.25 |
| CHEMBL285819 | — | — | 1 | 7.20 |
| CHEMBL411066 | KINETIN RIBOSIDE | — | 1 | 6.89 |
| CHEMBL2113392 | — | — | 1 | 6.79 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.54 |
| CHEMBL2113474 | — | — | 1 | 6.53 |
| CHEMBL2113396 | — | — | 1 | 6.24 |
| CHEMBL49843 | — | — | 1 | 6.22 |
| CHEMBL443485 | 5'-Deoxyadenosine | — | 1 | 6.22 |
| CHEMBL129014 | NORARISTEROMYCIN | — | 1 | 6.16 |
| CHEMBL3142980 | — | — | 1 | 6.05 |
| CHEMBL278932 | — | — | 1 | 5.74 |
| CHEMBL278403 | — | — | 1 | 5.37 |
| CHEMBL471144 | — | — | 1 | 5.30 |
| CHEMBL2113475 | — | — | 1 | 5.21 |
| CHEMBL2079570 | — | — | 1 | 5.15 |
| CHEMBL236757 | — | — | 1 | 5.13 |
| CHEMBL2051948 | — | — | 1 | 5.07 |
| CHEMBL2113394 | — | — | 1 | 5.00 |
| CHEMBL2113473 | — | — | 1 | 4.94 |
| CHEMBL17765 | — | — | 1 | 4.89 |
| CHEMBL1619 | CLADRIBINE | 4.0 | 1 | 4.69 |
| CHEMBL2112597 | — | — | 1 | 4.68 |
| CHEMBL1775009 | — | — | 1 | 4.64 |
| CHEMBL516197 | — | — | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL410873 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL464859 | NECA | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL2079643 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL1568 | FLUDARABINE | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL119709 | IB-MECA | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL285819 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL411066 | KINETIN RIBOSIDE | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL2113392 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL2113474 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL2113396 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL49843 | — | Ki | = | 597.0 | nM | 6.22 |
| CHEMBL443485 | 5'-Deoxyadenosine | Ki | = | 596.0 | nM | 6.22 |
| CHEMBL129014 | NORARISTEROMYCIN | Ki | = | 692.0 | nM | 6.16 |
| CHEMBL3142980 | — | Ki | = | 897.0 | nM | 6.05 |
| CHEMBL278932 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL278403 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL471144 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL2113475 | — | Ki | = | 6220.0 | nM | 5.21 |
| CHEMBL2079570 | — | Ki | = | 7120.0 | nM | 5.15 |
| CHEMBL236757 | — | Ki | = | 7340.0 | nM | 5.13 |
| CHEMBL2051948 | — | Ki | = | 8540.0 | nM | 5.07 |
| CHEMBL2113394 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL2113473 | — | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL17765 | — | Ki | = | 12800.0 | nM | 4.89 |
| CHEMBL1619 | CLADRIBINE | Ki | = | 20400.0 | nM | 4.69 |
| CHEMBL2112597 | — | Ki | = | 20800.0 | nM | 4.68 |
| CHEMBL1775009 | — | Ki | = | 22700.0 | nM | 4.64 |
| CHEMBL516197 | — | Ki | = | 24100.0 | nM | 4.62 |
| CHEMBL17875 | — | Ki | = | 41100.0 | nM | 4.39 |
| CHEMBL2113395 | — | Ki | = | 53600.0 | nM | 4.27 |
| CHEMBL275433 | — | Ki | = | 55500.0 | nM | 4.26 |
| CHEMBL202701 | — | Ki | = | 59800.0 | nM | 4.22 |