Assay Detail
Binding
CHEMBL637704
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Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand
29
Total Activities
29
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
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 | 6.96 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 8.92 |
| CHEMBL2113503 | — | — | 1 | 8.00 |
| CHEMBL464859 | NECA | — | 1 | 7.88 |
| CHEMBL2113512 | — | — | 1 | 7.73 |
| CHEMBL2113514 | — | — | 1 | 7.42 |
| CHEMBL2113508 | — | — | 1 | 7.16 |
| CHEMBL2113476 | — | — | 1 | 7.09 |
| CHEMBL2094089 | — | — | 1 | 6.99 |
| CHEMBL319387 | — | — | 1 | 6.90 |
| CHEMBL608309 | — | — | 1 | 6.89 |
| CHEMBL2113510 | — | — | 1 | 6.81 |
| CHEMBL2113507 | — | — | 1 | 6.77 |
| CHEMBL2113522 | — | — | 1 | 6.73 |
| CHEMBL2113496 | — | — | 1 | 6.70 |
| CHEMBL2113515 | — | — | 1 | 6.63 |
| CHEMBL2113513 | — | — | 1 | 6.61 |
| CHEMBL2113511 | — | — | 1 | 6.59 |
| CHEMBL607728 | — | — | 1 | 6.57 |
| CHEMBL1256672 | — | — | 1 | 6.11 |
| CHEMBL331372 | CGS-21680 | — | 1 | 5.91 |
| CHEMBL2113523 | — | — | 1 | 5.82 |
| CHEMBL609783 | — | — | 1 | - |
| CHEMBL612163 | — | — | 1 | - |
| CHEMBL606230 | — | — | 1 | - |
| CHEMBL606229 | — | — | 1 | - |
| CHEMBL609784 | — | — | 1 | - |
| CHEMBL315101 | — | — | 1 | - |
| CHEMBL609199 | — | — | 1 | - |
| CHEMBL612164 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL2113503 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL464859 | NECA | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL2113512 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL2113514 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL2113508 | — | Ki | = | 69.8 | nM | 7.16 |
| CHEMBL2113476 | — | Ki | = | 81.4 | nM | 7.09 |
| CHEMBL2094089 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL319387 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL608309 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL2113510 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL2113507 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2113522 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL2113496 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL2113515 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL2113513 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL2113511 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL607728 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL1256672 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL331372 | CGS-21680 | Ki | = | 1232.0 | nM | 5.91 |
| CHEMBL2113523 | — | Ki | = | 1498.0 | nM | 5.82 |
| CHEMBL609783 | — | Ki | > | 567.0 | nM | - |
| CHEMBL612163 | — | Ki | > | 567.0 | nM | - |
| CHEMBL606230 | — | Ki | > | 567.0 | nM | - |
| CHEMBL606229 | — | Ki | > | 567.0 | nM | - |
| CHEMBL609784 | — | Ki | > | 567.0 | nM | - |
| CHEMBL315101 | — | Ki | > | 567.0 | nM | - |
| CHEMBL609199 | — | Ki | > | 567.0 | nM | - |
| CHEMBL612164 | — | Ki | > | 567.0 | nM | - |