Assay Detail
Binding
CHEMBL642986
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Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 4 | 8.26 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 9.72 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.31 |
| CHEMBL84363 | — | — | 1 | 9.00 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL84363 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 9700.0 | nM | 5.01 |