Assay Detail
Binding
CHEMBL4426297
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Displacement of [3H]-ZM241385 from wild type human adenosine receptor A2a expressed in HEK293 cell membranes after 240 mins by scintillation counting
5
Total Activities
5
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 | Autocuration |
Publication
Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.74 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184061 | — | — | 1 | 9.48 |
| CHEMBL113142 | ZM-241385 | — | 1 | 9.40 |
| CHEMBL187810 | — | — | 1 | 8.89 |
| CHEMBL3937413 | — | — | 1 | 8.42 |
| CHEMBL3934661 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184061 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL113142 | ZM-241385 | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL187810 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3937413 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3934661 | — | Ki | = | 31.0 | nM | 7.51 |