Assay Detail
Binding
CHEMBL875796
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Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand.
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| 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 | 5.91 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1568 | FLUDARABINE | 3.0 | 1 | 8.23 |
| CHEMBL285819 | — | — | 1 | 8.03 |
| CHEMBL2113474 | — | — | 1 | 7.38 |
| CHEMBL2113396 | — | — | 1 | 7.29 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.27 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 7.22 |
| CHEMBL464859 | NECA | — | 1 | 7.20 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.92 |
| CHEMBL410873 | — | — | 1 | 6.89 |
| CHEMBL2113392 | — | — | 1 | 6.65 |
| CHEMBL411066 | KINETIN RIBOSIDE | — | 1 | 6.63 |
| CHEMBL443485 | 5'-Deoxyadenosine | — | 1 | 6.57 |
| CHEMBL2079643 | — | — | 1 | 6.52 |
| CHEMBL3142980 | — | — | 1 | 6.19 |
| CHEMBL49843 | — | — | 1 | 6.05 |
| CHEMBL278932 | — | — | 1 | 6.02 |
| CHEMBL471144 | — | — | 1 | 5.99 |
| CHEMBL2079570 | — | — | 1 | 5.27 |
| CHEMBL1619 | CLADRIBINE | 4.0 | 1 | 5.13 |
| CHEMBL17765 | — | — | 1 | 5.10 |
| CHEMBL2113475 | — | — | 1 | 5.07 |
| CHEMBL2113394 | — | — | 1 | 5.03 |
| CHEMBL2113473 | — | — | 1 | 4.94 |
| CHEMBL202701 | — | — | 1 | 4.67 |
| CHEMBL3142967 | — | — | 1 | 4.54 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 4.54 |
| CHEMBL236757 | — | — | 1 | 4.53 |
| CHEMBL129014 | NORARISTEROMYCIN | — | 1 | 4.48 |
| CHEMBL17857 | — | — | 1 | 4.45 |
| CHEMBL480143 | — | — | 1 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1568 | FLUDARABINE | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL285819 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL2113474 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2113396 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL119709 | IB-MECA | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 59.6 | nM | 7.22 |
| CHEMBL464859 | NECA | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL410873 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2113392 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL411066 | KINETIN RIBOSIDE | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL443485 | 5'-Deoxyadenosine | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL2079643 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3142980 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL49843 | — | Ki | = | 898.0 | nM | 6.05 |
| CHEMBL278932 | — | Ki | = | 946.0 | nM | 6.02 |
| CHEMBL471144 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL2079570 | — | Ki | = | 5360.0 | nM | 5.27 |
| CHEMBL1619 | CLADRIBINE | Ki | = | 7320.0 | nM | 5.13 |
| CHEMBL17765 | — | Ki | = | 7990.0 | nM | 5.10 |
| CHEMBL2113475 | — | Ki | = | 8610.0 | nM | 5.07 |
| CHEMBL2113394 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL2113473 | — | Ki | = | 11400.0 | nM | 4.94 |
| CHEMBL202701 | — | Ki | = | 21500.0 | nM | 4.67 |
| CHEMBL3142967 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL477 | ADENOSINE | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL236757 | — | Ki | = | 29700.0 | nM | 4.53 |
| CHEMBL129014 | NORARISTEROMYCIN | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL17857 | — | Ki | = | 35900.0 | nM | 4.45 |
| CHEMBL480143 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL2113395 | — | Ki | = | 62400.0 | nM | 4.21 |
| CHEMBL2051948 | — | Ki | = | 180000.0 | nM | - |
| CHEMBL275433 | — | Ki | = | 101000.0 | nM | - |
| CHEMBL267099 | TUBERCIDIN | Ki | > | 100000.0 | nM | - |