Assay Detail
Binding
CHEMBL640360
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Binding affinity towards adenosine A1 receptor was determined using radioligand [3H]CHA in whole rat brain membranes at 25 degree C
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.15 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262984 | — | — | 1 | 8.16 |
| CHEMBL128092 | — | — | 1 | 7.63 |
| CHEMBL128804 | — | — | 1 | 7.60 |
| CHEMBL337073 | — | — | 1 | 7.49 |
| CHEMBL339270 | — | — | 1 | 7.47 |
| CHEMBL130779 | — | — | 1 | 7.31 |
| CHEMBL340019 | — | — | 1 | 7.22 |
| CHEMBL132441 | — | — | 1 | 7.19 |
| CHEMBL336847 | — | — | 1 | 7.13 |
| CHEMBL128475 | — | — | 1 | 7.03 |
| CHEMBL423513 | — | — | 1 | 7.02 |
| CHEMBL128606 | — | — | 1 | 6.87 |
| CHEMBL132063 | — | — | 1 | 6.79 |
| CHEMBL2367993 | — | — | 1 | 6.78 |
| CHEMBL336189 | — | — | 1 | 6.76 |
| CHEMBL337294 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262984 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL128092 | — | Ki | = | 23.2 | nM | 7.63 |
| CHEMBL128804 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL337073 | — | Ki | = | 32.6 | nM | 7.49 |
| CHEMBL339270 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL130779 | — | Ki | = | 49.4 | nM | 7.31 |
| CHEMBL340019 | — | Ki | = | 60.7 | nM | 7.22 |
| CHEMBL132441 | — | Ki | = | 64.3 | nM | 7.19 |
| CHEMBL336847 | — | Ki | = | 73.8 | nM | 7.13 |
| CHEMBL128475 | — | Ki | = | 94.3 | nM | 7.03 |
| CHEMBL423513 | — | Ki | = | 94.6 | nM | 7.02 |
| CHEMBL128606 | — | Ki | = | 136.1 | nM | 6.87 |
| CHEMBL132063 | — | Ki | = | 161.2 | nM | 6.79 |
| CHEMBL2367993 | — | Ki | = | 164.3 | nM | 6.78 |
| CHEMBL336189 | — | Ki | = | 174.7 | nM | 6.76 |
| CHEMBL337294 | — | Ki | = | 1294.0 | nM | 5.89 |