Assay Detail
Binding
CHEMBL646355
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Binding affinity at Adenosine A2A receptor in rat striatal membrane by [3H]ZM-241385 displacement.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.56 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319387 | — | — | 1 | 8.22 |
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL2113592 | — | — | 1 | 7.70 |
| CHEMBL2113595 | — | — | 1 | 7.22 |
| CHEMBL2113605 | — | — | 1 | 6.96 |
| CHEMBL2113604 | — | — | 1 | 6.77 |
| CHEMBL2113601 | — | — | 1 | 6.66 |
| CHEMBL2113588 | — | — | 1 | 6.66 |
| CHEMBL2113593 | — | — | 1 | 6.36 |
| CHEMBL2113580 | — | — | 1 | 6.30 |
| CHEMBL2113582 | — | — | 1 | 6.09 |
| CHEMBL2113600 | — | — | 1 | 5.92 |
| CHEMBL2113581 | — | — | 1 | 5.82 |
| CHEMBL2113606 | — | — | 1 | 5.75 |
| CHEMBL2113602 | — | — | 1 | 5.41 |
| CHEMBL2113519 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319387 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2113592 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2113595 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2113605 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2113604 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL2113601 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL2113588 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL2113593 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL2113580 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2113582 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL2113600 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2113581 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2113606 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL2113602 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL2113519 | — | Ki | = | 4200.0 | nM | 5.38 |