Assay Detail
Binding
CHEMBL4259137
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Binding affinity to human adenosine A2A receptor by radioligand displacement assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.26 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 7.92 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 6.97 |
| CHEMBL320872 | — | — | 1 | 6.01 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.77 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL320872 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL113 | CAFFEINE | Ki | = | 23400.0 | nM | 4.63 |