Assay Detail
Binding
CHEMBL640561
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Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A1 receptor
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 9.06 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298474 | — | — | 3 | 9.35 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 9.14 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298474 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL298474 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL298474 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 2.52 | nM | 8.60 |