Assay Detail
Binding
CHEMBL636768
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against Adenosine A1 receptor in rat brain membrane, using [3H]N6-cyclohexyladenosine as the radioligand
22
Total Activities
22
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
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 5.88 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11348 | — | — | 1 | 7.36 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.07 |
| CHEMBL72117 | — | — | 1 | 6.91 |
| CHEMBL312447 | — | — | 1 | 6.76 |
| CHEMBL73582 | — | — | 1 | 6.75 |
| CHEMBL310535 | — | — | 1 | 6.53 |
| CHEMBL72125 | — | — | 1 | 6.35 |
| CHEMBL157655 | — | — | 1 | 6.35 |
| CHEMBL306389 | — | — | 1 | 6.21 |
| CHEMBL309026 | — | — | 1 | 6.07 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | — | 1 | 5.60 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.07 |
| CHEMBL73268 | — | — | 1 | 4.99 |
| CHEMBL419812 | — | — | 1 | 4.94 |
| CHEMBL72040 | — | — | 1 | 4.87 |
| CHEMBL72425 | — | — | 1 | 4.82 |
| CHEMBL307175 | — | — | 1 | 4.62 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.54 |
| CHEMBL72254 | — | — | 1 | - |
| CHEMBL72041 | — | — | 1 | - |
| CHEMBL73952 | — | — | 1 | - |
| CHEMBL74063 | ISOCAFFIENE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11348 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL72117 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL312447 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL73582 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL310535 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL72125 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL157655 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL306389 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL309026 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL73268 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL419812 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL72040 | — | Ki | = | 13400.0 | nM | 4.87 |
| CHEMBL72425 | — | Ki | = | 15200.0 | nM | 4.82 |
| CHEMBL307175 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL113 | CAFFEINE | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL72254 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL72041 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL73952 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL74063 | ISOCAFFIENE | Ki | = | 1000000.0 | nM | - |