Assay Detail
Binding
CHEMBL3708008
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Binding Assay: The affinities of selected Purine Derivatives for the adenosine A1 receptor were determined by measuring the displacement of specific [3H] 2-chloro-N6-cyclopentyl adenosine binding in CHO cells stably transfected with human recombinant A1 adenosine receptor expressed as Ki (nM).
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Purine derivatives as adenosine A1 receptor agonists and methods of use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.14 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2205239 | — | — | 1 | 6.67 |
| CHEMBL3642150 | — | — | 1 | 6.29 |
| CHEMBL3545407 | TRABODENOSON | 3.0 | 1 | 6.15 |
| CHEMBL3642983 | — | — | 1 | 6.05 |
| CHEMBL3642984 | — | — | 1 | 5.99 |
| CHEMBL3642152 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2205239 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL3642150 | — | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL3545407 | TRABODENOSON | Ki | = | 704.0 | nM | 6.15 |
| CHEMBL3642983 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3642984 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL3642152 | — | Ki | = | 2020.0 | nM | 5.70 |