Assay Detail
Binding
CHEMBL642305
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Binding affinity for adenosine A1 receptor as displacement of [3H]R-PIA from rat brain membranes at 10e-4 M
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.28 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL133566 | — | — | 1 | 8.47 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.27 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.09 |
| CHEMBL265096 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL133566 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL119709 | IB-MECA | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL265096 | — | Ki | > | 100000.0 | nM | - |