Assay Detail
Binding
CHEMBL636644
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Inhibition of [3H]CHA binding to Adenosine A1 receptor in rat brain membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.14 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273671 | — | — | 1 | 8.32 |
| CHEMBL268071 | — | — | 1 | 8.14 |
| CHEMBL16687 | CGS-15943 | — | 1 | 7.68 |
| CHEMBL301814 | — | — | 1 | 6.51 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273671 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL268071 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL16687 | CGS-15943 | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL301814 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 8500.0 | nM | 5.07 |