Assay Detail
Binding
CHEMBL645447
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Binding affinity against adenosine A2 receptor in rat striatal membranes using [3H]NECA as radioligand
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Nucleosides and nucleotides. 103. 2-Alkynyladenosines: a novel class of selective adenosine A2 receptor agonists with potent antihypertensive effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.54 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319387 | — | — | 1 | 8.55 |
| CHEMBL2113507 | — | — | 1 | 8.27 |
| CHEMBL2094089 | — | — | 1 | 8.16 |
| CHEMBL2113510 | — | — | 1 | 8.12 |
| CHEMBL331372 | CGS-21680 | — | 1 | 8.06 |
| CHEMBL608309 | — | — | 1 | 7.99 |
| CHEMBL2113512 | — | — | 1 | 7.97 |
| CHEMBL2113496 | — | — | 1 | 7.92 |
| CHEMBL464859 | NECA | — | 1 | 7.91 |
| CHEMBL2113513 | — | — | 1 | 7.89 |
| CHEMBL2113503 | — | — | 1 | 7.69 |
| CHEMBL2113522 | — | — | 1 | 7.67 |
| CHEMBL2113515 | — | — | 1 | 7.48 |
| CHEMBL2113511 | — | — | 1 | 7.47 |
| CHEMBL607728 | — | — | 1 | 7.42 |
| CHEMBL2113476 | — | — | 1 | 7.40 |
| CHEMBL2113514 | — | — | 1 | 7.05 |
| CHEMBL1256672 | — | — | 1 | 6.97 |
| CHEMBL609784 | — | — | 1 | 6.82 |
| CHEMBL2113523 | — | — | 1 | 6.51 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.38 |
| CHEMBL2113508 | — | — | 1 | 6.20 |
| CHEMBL606229 | — | — | 1 | - |
| CHEMBL609783 | — | — | 1 | - |
| CHEMBL612163 | — | — | 1 | - |
| CHEMBL606230 | — | — | 1 | - |
| CHEMBL609199 | — | — | 1 | - |
| CHEMBL315101 | — | — | 1 | - |
| CHEMBL612164 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319387 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2113507 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2094089 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL2113510 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL331372 | CGS-21680 | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL608309 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL2113512 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL2113496 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL464859 | NECA | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL2113513 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL2113503 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL2113522 | — | Ki | = | 21.2 | nM | 7.67 |
| CHEMBL2113515 | — | Ki | = | 32.8 | nM | 7.48 |
| CHEMBL2113511 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL607728 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL2113476 | — | Ki | = | 40.1 | nM | 7.40 |
| CHEMBL2113514 | — | Ki | = | 88.1 | nM | 7.05 |
| CHEMBL1256672 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL609784 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2113523 | — | Ki | = | 307.0 | nM | 6.51 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 421.0 | nM | 6.38 |
| CHEMBL2113508 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL606229 | — | Ki | > | 567.0 | nM | - |
| CHEMBL609783 | — | Ki | > | 567.0 | nM | - |
| CHEMBL612163 | — | Ki | > | 567.0 | nM | - |
| CHEMBL606230 | — | Ki | > | 567.0 | nM | - |
| CHEMBL609199 | — | Ki | > | 567.0 | nM | - |
| CHEMBL315101 | — | Ki | > | 567.0 | nM | - |
| CHEMBL612164 | — | Ki | > | 567.0 | nM | - |