Assay Detail
Binding
CHEMBL5148528
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]HEMADO from human A3AR expressed in CHO-K1 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]HEMADO addition and measured after 1.5 hrs by TopCount scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Benzo[4,5]imidazo[1,2-<i>a</i>]pyrazin-1-amine-3-amide-one Derivatives as Anticancer Human A<sub>2A</sub> Adenosine Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 5.35 | 5.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5203105 | — | — | 1 | 5.90 |
| CHEMBL5176737 | — | — | 1 | 5.51 |
| CHEMBL4594442 | IMARADENANT | 2.0 | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5203105 | — | Ki | = | 1261.2 | nM | 5.90 |
| CHEMBL5176737 | — | Ki | = | 3052.2 | nM | 5.51 |
| CHEMBL4594442 | IMARADENANT | Ki | = | 22685.8 | nM | 4.64 |