Assay Detail
Binding
CHEMBL4737366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ZM241385 from recombinant human A2A receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.02 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4742132 | — | — | 1 | 8.62 |
| CHEMBL4746388 | — | — | 1 | 8.55 |
| CHEMBL4753657 | — | — | 1 | 8.44 |
| CHEMBL4784681 | — | — | 1 | 8.44 |
| CHEMBL4783617 | — | — | 1 | 8.42 |
| CHEMBL2105747 | TOZADENANT | 3.0 | 1 | 8.41 |
| CHEMBL4783723 | — | — | 1 | 8.31 |
| CHEMBL4750049 | — | — | 1 | 8.22 |
| CHEMBL4785362 | — | — | 1 | 8.19 |
| CHEMBL4746896 | — | — | 1 | 8.19 |
| CHEMBL4745912 | — | — | 1 | 8.03 |
| CHEMBL4748372 | — | — | 1 | 7.62 |
| CHEMBL4763600 | — | — | 1 | 7.48 |
| CHEMBL4795658 | — | — | 1 | 7.46 |
| CHEMBL4788835 | — | — | 1 | 7.42 |
| CHEMBL4760845 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4742132 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL4746388 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL4753657 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4784681 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4783617 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2105747 | TOZADENANT | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4783723 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL4750049 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4785362 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL4746896 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL4745912 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL4748372 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL4763600 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4795658 | — | Ki | = | 35.1 | nM | 7.46 |
| CHEMBL4788835 | — | Ki | = | 37.9 | nM | 7.42 |
| CHEMBL4760845 | — | Ki | = | 361.0 | nM | 6.44 |