Assay Detail
Binding
CHEMBL646482
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Binding affinity towards adenosine A2 receptor in rat striatal membranes using N-[3H]-ethyladenosin-5''-uronamide as radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.66 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | — | 1 | 8.48 |
| CHEMBL308499 | — | — | 1 | 7.81 |
| CHEMBL303198 | — | — | 1 | 7.68 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.20 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.39 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.07 |
| CHEMBL268071 | — | — | 1 | 6.00 |
| CHEMBL72669 | — | — | 1 | 5.68 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL308499 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL303198 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 848.0 | nM | 6.07 |
| CHEMBL268071 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL72669 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 25300.0 | nM | 4.60 |