Assay Detail
Binding
CHEMBL649876
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Binding affinity against Adenosine A2 receptor in rat brain membrane, using [3H]-NECA as the radioligand.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.17 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL73582 | — | — | 1 | 6.17 |
| CHEMBL310535 | — | — | 1 | 6.10 |
| CHEMBL11348 | — | — | 1 | 6.07 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.07 |
| CHEMBL72117 | — | — | 1 | 5.88 |
| CHEMBL312447 | — | — | 1 | 5.71 |
| CHEMBL309026 | — | — | 1 | 5.71 |
| CHEMBL306389 | — | — | 1 | 5.62 |
| CHEMBL157655 | — | — | 1 | 5.28 |
| CHEMBL72125 | — | — | 1 | 4.98 |
| CHEMBL73268 | — | — | 1 | 4.90 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | — | 1 | 4.86 |
| CHEMBL72040 | — | — | 1 | 4.75 |
| CHEMBL419812 | — | — | 1 | 4.64 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.60 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.32 |
| CHEMBL72425 | — | — | 1 | 4.24 |
| CHEMBL73952 | — | — | 1 | 4.24 |
| CHEMBL307175 | — | — | 1 | 4.07 |
| CHEMBL72041 | — | — | 1 | - |
| CHEMBL72254 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL73582 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL310535 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL11348 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL72117 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL312447 | — | Ki | = | 1960.0 | nM | 5.71 |
| CHEMBL309026 | — | Ki | = | 1970.0 | nM | 5.71 |
| CHEMBL306389 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL157655 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL72125 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL73268 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | Ki | = | 13800.0 | nM | 4.86 |
| CHEMBL72040 | — | Ki | = | 17900.0 | nM | 4.75 |
| CHEMBL419812 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL113 | CAFFEINE | Ki | = | 48000.0 | nM | 4.32 |
| CHEMBL72425 | — | Ki | = | 58000.0 | nM | 4.24 |
| CHEMBL73952 | — | Ki | = | 58000.0 | nM | 4.24 |
| CHEMBL307175 | — | Ki | = | 85000.0 | nM | 4.07 |
| CHEMBL72041 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL72254 | — | Ki | > | 100000.0 | nM | - |