Assay Detail
Functional
CHEMBL927306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at adenosine A1 receptor in pig cortical membrane assessed as stimulation of GTPgammaS binding
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 9 | 6.50 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 8.10 |
| CHEMBL252198 | — | — | 1 | 7.74 |
| CHEMBL392149 | TECADENOSON | 2.0 | 1 | 7.50 |
| CHEMBL254064 | — | — | 1 | 6.78 |
| CHEMBL399514 | — | — | 1 | 6.49 |
| CHEMBL254483 | — | — | 1 | 5.62 |
| CHEMBL400782 | — | — | 1 | 5.56 |
| CHEMBL400190 | — | — | 1 | 5.44 |
| CHEMBL400330 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL252198 | — | EC50 | = | 18.3 | nM | 7.74 |
| CHEMBL392149 | TECADENOSON | EC50 | = | 31.6 | nM | 7.50 |
| CHEMBL254064 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL399514 | — | EC50 | = | 326.0 | nM | 6.49 |
| CHEMBL254483 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL400782 | — | EC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL400190 | — | EC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL400330 | — | EC50 | = | 5000.0 | nM | 5.30 |