Assay Detail
Binding
CHEMBL636765
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Binding affinity against Adenosine A1 receptor by displacing [3H]CHA radioligand in rat brain cortical membrane
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| 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 | 27 | 5.15 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.05 |
| CHEMBL1788234 | — | — | 1 | 6.94 |
| CHEMBL118044 | — | — | 1 | 6.58 |
| CHEMBL1625681 | — | — | 1 | 6.36 |
| CHEMBL282993 | — | — | 1 | 6.19 |
| CHEMBL1744045 | — | — | 1 | 6.14 |
| CHEMBL1788230 | — | — | 1 | 6.02 |
| CHEMBL117962 | — | — | 1 | 5.74 |
| CHEMBL26897 | — | — | 1 | 5.41 |
| CHEMBL2112319 | — | — | 1 | 5.33 |
| CHEMBL118082 | — | — | 1 | 5.21 |
| CHEMBL117899 | — | — | 1 | 5.01 |
| CHEMBL323615 | — | — | 1 | 4.98 |
| CHEMBL2111766 | — | — | 1 | 4.83 |
| CHEMBL21053 | — | — | 1 | 4.82 |
| CHEMBL1788235 | — | — | 1 | 4.76 |
| CHEMBL116382 | — | — | 1 | 4.70 |
| CHEMBL2112561 | — | — | 1 | 4.66 |
| CHEMBL1788233 | — | — | 1 | 4.64 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.39 |
| CHEMBL323723 | — | — | 1 | 4.37 |
| CHEMBL117999 | — | — | 1 | 4.23 |
| CHEMBL117513 | — | — | 1 | 4.22 |
| CHEMBL326789 | — | — | 1 | 4.18 |
| CHEMBL2112320 | — | — | 1 | 4.16 |
| CHEMBL2112318 | — | — | 1 | 4.12 |
| CHEMBL325043 | — | — | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL1788234 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL118044 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL1625681 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL282993 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL1744045 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL1788230 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL117962 | — | Ki | = | 1830.0 | nM | 5.74 |
| CHEMBL26897 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL2112319 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL118082 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL117899 | — | Ki | = | 9700.0 | nM | 5.01 |
| CHEMBL323615 | — | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL2111766 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL21053 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL1788235 | — | Ki | = | 17500.0 | nM | 4.76 |
| CHEMBL116382 | — | Ki | = | 19800.0 | nM | 4.70 |
| CHEMBL2112561 | — | Ki | = | 21700.0 | nM | 4.66 |
| CHEMBL1788233 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL113 | CAFFEINE | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL323723 | — | Ki | = | 43200.0 | nM | 4.37 |
| CHEMBL117999 | — | Ki | = | 59000.0 | nM | 4.23 |
| CHEMBL117513 | — | Ki | = | 60300.0 | nM | 4.22 |
| CHEMBL326789 | — | Ki | = | 65500.0 | nM | 4.18 |
| CHEMBL2112320 | — | Ki | = | 70000.0 | nM | 4.16 |
| CHEMBL2112318 | — | Ki | = | 75500.0 | nM | 4.12 |
| CHEMBL325043 | — | Ki | = | 79600.0 | nM | 4.10 |