Assay Detail
Binding
CHEMBL4426296
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Displacement of [3H]-ZM241385 from human adenosine receptor A2a StaR2-bRIL mutant 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 | 0 — Uncurated / Unknown |
| 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 | 8.85 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184061 | — | — | 1 | 9.46 |
| CHEMBL113142 | ZM-241385 | — | 1 | 9.28 |
| CHEMBL3937413 | — | — | 1 | 8.96 |
| CHEMBL187810 | — | — | 1 | 8.82 |
| CHEMBL3934661 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184061 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL113142 | ZM-241385 | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL3937413 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL187810 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3934661 | — | Ki | = | 18.0 | nM | 7.75 |