Assay Detail
Binding
CHEMBL646279
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Binding affinity to the adenosine A2A receptor by displacement of [3H]CGS-21680 in rat brain striatal membrane
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.13 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26897 | — | — | 1 | 7.03 |
| CHEMBL282993 | — | — | 1 | 6.54 |
| CHEMBL2111766 | — | — | 1 | 6.37 |
| CHEMBL2112561 | — | — | 1 | 6.26 |
| CHEMBL1744045 | — | — | 1 | 6.17 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.08 |
| CHEMBL1788230 | — | — | 1 | 6.05 |
| CHEMBL1625681 | — | — | 1 | 5.68 |
| CHEMBL118044 | — | — | 1 | 5.51 |
| CHEMBL1788234 | — | — | 1 | 5.48 |
| CHEMBL1788229 | — | — | 1 | 4.96 |
| CHEMBL2112320 | — | — | 1 | 4.92 |
| CHEMBL323615 | — | — | 1 | 4.92 |
| CHEMBL117962 | — | — | 1 | 4.92 |
| CHEMBL117317 | — | — | 1 | 4.79 |
| CHEMBL432242 | — | — | 1 | 4.79 |
| CHEMBL2112319 | — | — | 1 | 4.79 |
| CHEMBL116382 | — | — | 1 | 4.73 |
| CHEMBL118082 | — | — | 1 | 4.72 |
| CHEMBL117899 | — | — | 1 | 4.69 |
| CHEMBL325043 | — | — | 1 | 4.68 |
| CHEMBL21053 | — | — | 1 | 4.60 |
| CHEMBL2112318 | — | — | 1 | 4.55 |
| CHEMBL323723 | — | — | 1 | 4.54 |
| CHEMBL1788235 | — | — | 1 | 4.44 |
| CHEMBL326789 | — | — | 1 | 4.39 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.37 |
| CHEMBL1788233 | — | — | 1 | 4.30 |
| CHEMBL117513 | — | — | 1 | 4.29 |
| CHEMBL117999 | — | — | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26897 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL282993 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL2111766 | — | Ki | = | 424.0 | nM | 6.37 |
| CHEMBL2112561 | — | Ki | = | 547.0 | nM | 6.26 |
| CHEMBL1744045 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL1788230 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL1625681 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL118044 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL1788234 | — | Ki | = | 3330.0 | nM | 5.48 |
| CHEMBL1788229 | — | Ki | = | 10900.0 | nM | 4.96 |
| CHEMBL2112320 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL323615 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL117962 | — | Ki | = | 11900.0 | nM | 4.92 |
| CHEMBL117317 | — | Ki | = | 16100.0 | nM | 4.79 |
| CHEMBL432242 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL2112319 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL116382 | — | Ki | = | 18500.0 | nM | 4.73 |
| CHEMBL118082 | — | Ki | = | 19200.0 | nM | 4.72 |
| CHEMBL117899 | — | Ki | = | 20300.0 | nM | 4.69 |
| CHEMBL325043 | — | Ki | = | 20700.0 | nM | 4.68 |
| CHEMBL21053 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL2112318 | — | Ki | = | 28300.0 | nM | 4.55 |
| CHEMBL323723 | — | Ki | = | 28500.0 | nM | 4.54 |
| CHEMBL1788235 | — | Ki | = | 36300.0 | nM | 4.44 |
| CHEMBL326789 | — | Ki | = | 40900.0 | nM | 4.39 |
| CHEMBL113 | CAFFEINE | Ki | = | 43000.0 | nM | 4.37 |
| CHEMBL1788233 | — | Ki | = | 50400.0 | nM | 4.30 |
| CHEMBL117513 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL117999 | — | Ki | = | 64600.0 | nM | 4.19 |