Assay Detail
Binding
CHEMBL2328345
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Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.47 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2326828 | — | — | 1 | 7.92 |
| CHEMBL464859 | NECA | — | 1 | 7.82 |
| CHEMBL2326842 | — | — | 1 | 7.79 |
| CHEMBL331372 | CGS-21680 | — | 1 | 7.75 |
| CHEMBL2326843 | — | — | 1 | 7.61 |
| CHEMBL1950554 | BINODENOSON | 3.0 | 1 | 7.59 |
| CHEMBL2326829 | — | — | 1 | 7.27 |
| CHEMBL2326844 | — | — | 1 | 7.04 |
| CHEMBL2326831 | — | — | 1 | 6.48 |
| CHEMBL2326840 | — | — | 1 | - |
| CHEMBL2326839 | — | — | 1 | - |
| CHEMBL2326838 | — | — | 1 | - |
| CHEMBL2326837 | — | — | 1 | - |
| CHEMBL2326836 | — | — | 1 | - |
| CHEMBL2326835 | — | — | 1 | - |
| CHEMBL2326834 | — | — | 1 | - |
| CHEMBL2326833 | — | — | 1 | - |
| CHEMBL2326830 | — | — | 1 | - |
| CHEMBL2326841 | — | — | 1 | - |
| CHEMBL2326832 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2326828 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL464859 | NECA | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2326842 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL331372 | CGS-21680 | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2326843 | — | Ki | = | 24.4 | nM | 7.61 |
| CHEMBL1950554 | BINODENOSON | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL2326829 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL2326844 | — | Ki | = | 91.7 | nM | 7.04 |
| CHEMBL2326831 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL2326840 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326839 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326838 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326837 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326836 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326835 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326834 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326833 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326830 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326841 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2326832 | — | Ki | > | 1000.0 | nM | - |