Assay Detail
Binding
CHEMBL642336
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Binding affinity towards adenosine A2 receptor was determined using radioligand [3H]NECA in rat brain striatum at 25 degree C
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.57 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262984 | — | — | 1 | 6.80 |
| CHEMBL336847 | — | — | 1 | 6.21 |
| CHEMBL337073 | — | — | 1 | 6.19 |
| CHEMBL340019 | — | — | 1 | 6.07 |
| CHEMBL132063 | — | — | 1 | 5.91 |
| CHEMBL128475 | — | — | 1 | 5.76 |
| CHEMBL2367993 | — | — | 1 | 5.57 |
| CHEMBL339270 | — | — | 1 | 5.49 |
| CHEMBL128092 | — | — | 1 | 5.46 |
| CHEMBL128804 | — | — | 1 | 5.38 |
| CHEMBL130779 | — | — | 1 | 5.31 |
| CHEMBL128606 | — | — | 1 | 5.12 |
| CHEMBL132441 | — | — | 1 | 5.08 |
| CHEMBL423513 | — | — | 1 | 4.99 |
| CHEMBL337294 | — | — | 1 | 4.89 |
| CHEMBL336189 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262984 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL336847 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL337073 | — | Ki | = | 644.0 | nM | 6.19 |
| CHEMBL340019 | — | Ki | = | 848.0 | nM | 6.07 |
| CHEMBL132063 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL128475 | — | Ki | = | 1740.0 | nM | 5.76 |
| CHEMBL2367993 | — | Ki | = | 2720.0 | nM | 5.57 |
| CHEMBL339270 | — | Ki | = | 3210.0 | nM | 5.49 |
| CHEMBL128092 | — | Ki | = | 3510.0 | nM | 5.46 |
| CHEMBL128804 | — | Ki | = | 4220.0 | nM | 5.38 |
| CHEMBL130779 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL128606 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL132441 | — | Ki | = | 8350.0 | nM | 5.08 |
| CHEMBL423513 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL337294 | — | Ki | = | 12800.0 | nM | 4.89 |
| CHEMBL336189 | — | Ki | = | 12900.0 | nM | 4.89 |