Assay Detail
Binding
CHEMBL927300
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Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.59 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284969 | — | — | 1 | 9.52 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.28 |
| CHEMBL251997 | — | — | 1 | 8.44 |
| CHEMBL252198 | — | — | 1 | 8.18 |
| CHEMBL392149 | TECADENOSON | 2.0 | 1 | 8.12 |
| CHEMBL400189 | — | — | 1 | 8.00 |
| CHEMBL399514 | — | — | 1 | 7.89 |
| CHEMBL400782 | — | — | 1 | 7.17 |
| CHEMBL254064 | — | — | 1 | 7.14 |
| CHEMBL400190 | — | — | 1 | 6.82 |
| CHEMBL254483 | — | — | 1 | 6.76 |
| CHEMBL254896 | — | — | 1 | 6.56 |
| CHEMBL254270 | — | — | 1 | 6.47 |
| CHEMBL427718 | — | — | 1 | 6.43 |
| CHEMBL254481 | — | — | 1 | 6.42 |
| CHEMBL254271 | — | — | 1 | 6.42 |
| CHEMBL400330 | — | — | 1 | 6.39 |
| CHEMBL254065 | — | — | 1 | 6.29 |
| CHEMBL254693 | — | — | 1 | 6.27 |
| CHEMBL254482 | — | — | 1 | 6.12 |
| CHEMBL399306 | — | — | 1 | 5.99 |
| CHEMBL254897 | — | — | 1 | 5.84 |
| CHEMBL398544 | — | — | 1 | 5.73 |
| CHEMBL429667 | — | — | 1 | 5.73 |
| CHEMBL254063 | — | — | 1 | 5.69 |
| CHEMBL251799 | — | — | 1 | 5.69 |
| CHEMBL251798 | — | — | 1 | 5.54 |
| CHEMBL254691 | — | — | 1 | 5.50 |
| CHEMBL400331 | — | — | 1 | 5.41 |
| CHEMBL254898 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284969 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL251997 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL252198 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL392149 | TECADENOSON | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL400189 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL399514 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL400782 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL254064 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL400190 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL254483 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL254896 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL254270 | — | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL427718 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL254271 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL254481 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL400330 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL254065 | — | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL254693 | — | Ki | = | 534.0 | nM | 6.27 |
| CHEMBL254482 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL399306 | — | Ki | = | 1026.0 | nM | 5.99 |
| CHEMBL254897 | — | Ki | = | 1450.0 | nM | 5.84 |
| CHEMBL398544 | — | Ki | = | 1848.0 | nM | 5.73 |
| CHEMBL429667 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL254063 | — | Ki | = | 2052.0 | nM | 5.69 |
| CHEMBL251799 | — | Ki | = | 2053.0 | nM | 5.69 |
| CHEMBL251798 | — | Ki | = | 2870.0 | nM | 5.54 |
| CHEMBL254691 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL400331 | — | Ki | = | 3879.0 | nM | 5.41 |
| CHEMBL254898 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL398543 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL254692 | — | Ki | = | 16200.0 | nM | 4.79 |