Assay Detail
Binding
CHEMBL640352
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Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 6.09 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77717 | — | — | 1 | 8.89 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.19 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.96 |
| CHEMBL308499 | — | — | 1 | 6.85 |
| CHEMBL77435 | — | — | 1 | 6.50 |
| CHEMBL33115 | — | — | 1 | 6.25 |
| CHEMBL312079 | — | — | 1 | 6.14 |
| CHEMBL76482 | — | — | 1 | 6.09 |
| CHEMBL77279 | — | — | 1 | 6.07 |
| CHEMBL307942 | — | — | 1 | 6.06 |
| CHEMBL157655 | — | — | 1 | 5.92 |
| CHEMBL433113 | — | — | 1 | 5.89 |
| CHEMBL309719 | — | — | 1 | 5.89 |
| CHEMBL306633 | — | — | 1 | 5.85 |
| CHEMBL74368 | — | — | 1 | 5.85 |
| CHEMBL27508 | — | — | 1 | 5.82 |
| CHEMBL27496 | — | — | 1 | 5.77 |
| CHEMBL283908 | — | — | 1 | 5.75 |
| CHEMBL306313 | — | — | 1 | 5.68 |
| CHEMBL307805 | — | — | 1 | 5.64 |
| CHEMBL75597 | — | — | 1 | 5.46 |
| CHEMBL22099 | — | — | 1 | 5.09 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.64 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.00 |
| CHEMBL26979 | — | — | 1 | - |
| CHEMBL76844 | — | — | 1 | - |
| CHEMBL75093 | — | — | 1 | - |
| CHEMBL76540 | — | — | 1 | - |
| CHEMBL27203 | — | — | 1 | - |
| CHEMBL308496 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77717 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL308499 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL77435 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL33115 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL312079 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL76482 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL77279 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL307942 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL157655 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL433113 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL309719 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL306633 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL74368 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL27508 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL27496 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL283908 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL306313 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL307805 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL75597 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL22099 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL113 | CAFFEINE | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL76083 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL77323 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL307403 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL76585 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL27714 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL308496 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL27203 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL76540 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL75093 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL76844 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL26979 | — | Ki | > | 100000.0 | nM | - |