Assay Detail
Binding
CHEMBL642308
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Binding affinity towards adenosine A1 receptor in rat cerebral cortical membranes by [3H]cyclohexyladenosine displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.69 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 8.92 |
| CHEMBL286728 | — | — | 1 | 8.66 |
| CHEMBL27155 | — | — | 1 | 8.54 |
| CHEMBL444281 | — | — | 1 | 8.39 |
| CHEMBL422937 | — | — | 1 | 8.30 |
| CHEMBL27081 | — | — | 1 | 8.05 |
| CHEMBL265739 | — | — | 1 | 7.62 |
| CHEMBL441598 | — | — | 1 | 7.58 |
| CHEMBL27028 | — | — | 1 | 7.50 |
| CHEMBL432664 | — | — | 1 | 7.44 |
| CHEMBL27762 | — | — | 1 | 7.38 |
| CHEMBL27047 | — | — | 1 | 7.30 |
| CHEMBL283628 | — | — | 1 | 7.27 |
| CHEMBL27041 | — | — | 1 | 7.24 |
| CHEMBL286063 | — | — | 1 | 7.23 |
| CHEMBL286493 | — | — | 1 | 7.02 |
| CHEMBL285103 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL286728 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL27155 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL444281 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL422937 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL27081 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL265739 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL441598 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL27028 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL432664 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL27762 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL27047 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL283628 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL27041 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL286063 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL286493 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL285103 | — | Ki | = | 500.0 | nM | 6.30 |