Assay Detail
Binding
CHEMBL633041
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Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.24 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL331372 | CGS-21680 | — | 1 | 7.96 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 7.60 |
| CHEMBL139000 | (R)-PIA | — | 1 | 6.93 |
| CHEMBL327073 | — | — | 1 | 6.61 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 6.49 |
| CHEMBL2112564 | — | — | 1 | 6.20 |
| CHEMBL115471 | — | — | 1 | 5.96 |
| CHEMBL117974 | — | — | 1 | 5.94 |
| CHEMBL116903 | — | — | 1 | 5.89 |
| CHEMBL423315 | — | — | 1 | 5.83 |
| CHEMBL411732 | — | — | 1 | 5.38 |
| CHEMBL117904 | — | — | 1 | 5.24 |
| CHEMBL326838 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL331372 | CGS-21680 | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL139000 | (R)-PIA | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL327073 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 321.0 | nM | 6.49 |
| CHEMBL2112564 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL115471 | — | Ki | = | 1086.0 | nM | 5.96 |
| CHEMBL117974 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL116903 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL423315 | — | Ki | = | 1485.0 | nM | 5.83 |
| CHEMBL411732 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL117904 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL326838 | — | Ki | = | 7420.0 | nM | 5.13 |