Assay Detail
Binding
CHEMBL5148523
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ZM241385 from human A2AAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]ZM241385 addition and measured after 1.5 hrs by TopCount scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 29 | 8.42 | 10.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5203105 | — | — | 1 | 10.09 |
| CHEMBL5176737 | — | — | 1 | 9.52 |
| CHEMBL5208415 | — | — | 1 | 9.07 |
| CHEMBL5174275 | — | — | 1 | 8.82 |
| CHEMBL4594442 | IMARADENANT | 2.0 | 1 | 8.76 |
| CHEMBL5171148 | — | — | 1 | 8.75 |
| CHEMBL5204660 | — | — | 1 | 8.68 |
| CHEMBL5192183 | — | — | 1 | 8.65 |
| CHEMBL5208426 | — | — | 1 | 8.55 |
| CHEMBL5201253 | — | — | 1 | 8.54 |
| CHEMBL5177737 | — | — | 1 | 8.51 |
| CHEMBL5197159 | — | — | 1 | 8.48 |
| CHEMBL5169483 | — | — | 1 | 8.46 |
| CHEMBL5176476 | — | — | 1 | 8.45 |
| CHEMBL5194978 | — | — | 1 | 8.40 |
| CHEMBL5203021 | — | — | 1 | 8.36 |
| CHEMBL5197028 | — | — | 1 | 8.35 |
| CHEMBL5192099 | — | — | 1 | 8.33 |
| CHEMBL5184887 | — | — | 1 | 8.27 |
| CHEMBL5204801 | — | — | 1 | 8.27 |
| CHEMBL5177540 | — | — | 1 | 8.26 |
| CHEMBL5181565 | — | — | 1 | 8.19 |
| CHEMBL5185998 | — | — | 1 | 8.09 |
| CHEMBL5190972 | — | — | 1 | 8.08 |
| CHEMBL5192000 | — | — | 1 | 7.83 |
| CHEMBL5192379 | — | — | 1 | 7.78 |
| CHEMBL5206624 | — | — | 1 | 7.57 |
| CHEMBL5196586 | — | — | 1 | 7.55 |
| CHEMBL5198502 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5203105 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL5176737 | — | Ki | = | 0.302 | nM | 9.52 |
| CHEMBL5208415 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL5174275 | — | Ki | = | 1.51 | nM | 8.82 |
| CHEMBL4594442 | IMARADENANT | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL5171148 | — | Ki | = | 1.79 | nM | 8.75 |
| CHEMBL5204660 | — | Ki | = | 2.07 | nM | 8.68 |
| CHEMBL5192183 | — | Ki | = | 2.23 | nM | 8.65 |
| CHEMBL5208426 | — | Ki | = | 2.82 | nM | 8.55 |
| CHEMBL5201253 | — | Ki | = | 2.91 | nM | 8.54 |
| CHEMBL5177737 | — | Ki | = | 3.09 | nM | 8.51 |
| CHEMBL5197159 | — | Ki | = | 3.31 | nM | 8.48 |
| CHEMBL5169483 | — | Ki | = | 3.43 | nM | 8.46 |
| CHEMBL5176476 | — | Ki | = | 3.52 | nM | 8.45 |
| CHEMBL5194978 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL5203021 | — | Ki | = | 4.42 | nM | 8.36 |
| CHEMBL5197028 | — | Ki | = | 4.44 | nM | 8.35 |
| CHEMBL5192099 | — | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL5184887 | — | Ki | = | 5.34 | nM | 8.27 |
| CHEMBL5204801 | — | Ki | = | 5.33 | nM | 8.27 |
| CHEMBL5177540 | — | Ki | = | 5.47 | nM | 8.26 |
| CHEMBL5181565 | — | Ki | = | 6.44 | nM | 8.19 |
| CHEMBL5185998 | — | Ki | = | 8.05 | nM | 8.09 |
| CHEMBL5190972 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL5192000 | — | Ki | = | 14.64 | nM | 7.83 |
| CHEMBL5192379 | — | Ki | = | 16.59 | nM | 7.78 |
| CHEMBL5206624 | — | Ki | = | 26.94 | nM | 7.57 |
| CHEMBL5196586 | — | Ki | = | 28.29 | nM | 7.55 |
| CHEMBL5198502 | — | Ki | = | 40.04 | nM | 7.40 |