Assay Detail
Binding
CHEMBL646359
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Inhibition of binding of [3H]NECA to adenosine A2 receptor of rat striatal membranes.
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
C2,N6-disubstituted adenosines: synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 45 | 6.36 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2094089 | — | — | 1 | 8.36 |
| CHEMBL2181971 | — | — | 1 | 8.31 |
| CHEMBL606507 | — | — | 1 | 8.21 |
| CHEMBL132960 | — | — | 1 | 8.03 |
| CHEMBL605859 | — | — | 1 | 7.83 |
| CHEMBL604830 | — | — | 1 | 7.66 |
| CHEMBL193692 | — | — | 1 | 7.60 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.43 |
| CHEMBL285819 | — | — | 1 | 7.20 |
| CHEMBL1256672 | — | — | 1 | 6.94 |
| CHEMBL139000 | (R)-PIA | — | 1 | 6.91 |
| CHEMBL604861 | — | — | 1 | 6.87 |
| CHEMBL605035 | — | — | 1 | 6.84 |
| CHEMBL603353 | — | — | 1 | 6.64 |
| CHEMBL603568 | — | — | 1 | 6.62 |
| CHEMBL604621 | — | — | 1 | 6.57 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.55 |
| CHEMBL604825 | — | — | 1 | 6.47 |
| CHEMBL606494 | — | — | 1 | 6.46 |
| CHEMBL606071 | — | — | 1 | 6.35 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.34 |
| CHEMBL603995 | — | — | 1 | 6.33 |
| CHEMBL603572 | — | — | 1 | 6.33 |
| CHEMBL604206 | — | — | 1 | 6.21 |
| CHEMBL45891 | — | — | 1 | 6.21 |
| CHEMBL603352 | — | — | 1 | 6.19 |
| CHEMBL489640 | — | — | 1 | 6.11 |
| CHEMBL603787 | — | — | 1 | 6.10 |
| CHEMBL603786 | — | — | 1 | 6.02 |
| CHEMBL603992 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2094089 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2181971 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL606507 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL132960 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL605859 | — | Ki | = | 14.9 | nM | 7.83 |
| CHEMBL604830 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL193692 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL477 | ADENOSINE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL285819 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL1256672 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL139000 | (R)-PIA | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL604861 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL605035 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL603353 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL603568 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL604621 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL604825 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL606494 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL606071 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL603572 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL603995 | — | Ki | = | 472.0 | nM | 6.33 |
| CHEMBL604206 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL45891 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL603352 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL489640 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL603787 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL603786 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL603992 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL2113423 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL603991 | — | Ki | = | 1530.0 | nM | 5.82 |
| CHEMBL604619 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL605451 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL604409 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL605068 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL606496 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL605235 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL605661 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL604202 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL605450 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL604616 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL603785 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL341031 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL605238 | — | Ki | = | 58000.0 | nM | 4.24 |