Assay Detail
Binding
CHEMBL641818
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Displacement of [3H]DPCPX from CHO cell membrane expressing human Adenosine A1 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.78 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL323717 | — | — | 1 | 7.55 |
| CHEMBL114832 | — | — | 1 | 7.38 |
| CHEMBL322250 | — | — | 1 | 7.30 |
| CHEMBL326757 | — | — | 1 | 7.08 |
| CHEMBL326319 | — | — | 1 | 6.91 |
| CHEMBL113634 | — | — | 1 | 6.75 |
| CHEMBL113512 | — | — | 1 | 6.49 |
| CHEMBL112098 | — | — | 1 | 5.84 |
| CHEMBL112194 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL323717 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL114832 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL322250 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL326757 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL326319 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL113634 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL113512 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL112098 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL112194 | — | Ki | = | 2100.0 | nM | 5.68 |