Assay Detail
Binding
CHEMBL639434
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Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Nucleosides and nucleotides. 112. 2-(1-Hexyn-1-yl)adenosine-5'-uronamides: a new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.84 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139835 | CYPROTERONE ACETATE | 3.0 | 1 | 9.12 |
| CHEMBL464859 | NECA | — | 1 | 8.08 |
| CHEMBL609475 | — | — | 1 | 7.73 |
| CHEMBL2094089 | — | — | 1 | 7.19 |
| CHEMBL319387 | — | — | 1 | 6.99 |
| CHEMBL2113496 | — | — | 1 | 6.93 |
| CHEMBL2113532 | — | — | 1 | 6.87 |
| CHEMBL2113531 | — | — | 1 | 6.66 |
| CHEMBL410873 | — | — | 1 | 6.56 |
| CHEMBL1256672 | — | — | 1 | 6.28 |
| CHEMBL331372 | CGS-21680 | — | 1 | 5.94 |
| CHEMBL2113480 | — | — | 1 | 5.90 |
| CHEMBL609211 | — | — | 1 | 5.75 |
| CHEMBL2113481 | — | — | 1 | 5.71 |
| CHEMBL609762 | — | — | 1 | - |
| CHEMBL610635 | — | — | 1 | - |
| CHEMBL608033 | — | — | 1 | - |
| CHEMBL610345 | — | — | 1 | - |
| CHEMBL611259 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139835 | CYPROTERONE ACETATE | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL464859 | NECA | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL609475 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL2094089 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL319387 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL2113496 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL2113532 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL2113531 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL410873 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL1256672 | — | Ki | = | 529.0 | nM | 6.28 |
| CHEMBL331372 | CGS-21680 | Ki | = | 1138.0 | nM | 5.94 |
| CHEMBL2113480 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL609211 | — | Ki | = | 1785.0 | nM | 5.75 |
| CHEMBL2113481 | — | Ki | = | 1932.0 | nM | 5.71 |
| CHEMBL609762 | — | Ki | > | 472.0 | nM | - |
| CHEMBL610635 | — | Ki | > | 472.0 | nM | - |
| CHEMBL608033 | — | Ki | > | 472.0 | nM | - |
| CHEMBL610345 | — | Ki | > | 472.0 | nM | - |
| CHEMBL611259 | — | Ki | > | 472.0 | nM | - |