Assay Detail
Binding
CHEMBL1042903
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Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.14 | 7.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL577036 | — | — | 1 | 7.73 |
| CHEMBL568023 | — | — | 1 | 6.43 |
| CHEMBL577915 | — | — | 1 | 6.27 |
| CHEMBL577458 | — | — | 1 | 6.22 |
| CHEMBL568009 | — | — | 1 | 6.15 |
| CHEMBL576883 | — | — | 1 | 6.10 |
| CHEMBL576838 | — | — | 1 | 5.96 |
| CHEMBL578145 | — | — | 1 | 5.94 |
| CHEMBL577902 | — | — | 1 | 5.87 |
| CHEMBL578569 | — | — | 1 | 5.82 |
| CHEMBL567801 | — | — | 1 | 5.61 |
| CHEMBL578819 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL577036 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL568023 | — | Ki | = | 372.0 | nM | 6.43 |
| CHEMBL577915 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL577458 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL568009 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL576883 | — | Ki | = | 793.0 | nM | 6.10 |
| CHEMBL576838 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL578145 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL577902 | — | Ki | = | 1350.0 | nM | 5.87 |
| CHEMBL578569 | — | Ki | = | 1520.0 | nM | 5.82 |
| CHEMBL567801 | — | Ki | = | 2480.0 | nM | 5.61 |
| CHEMBL578819 | — | Ki | = | 2900.0 | nM | 5.54 |