Assay Detail
Binding
CHEMBL829623
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Binding affinity towards Adenosine A2A receptor of rat brain tissues using [3H]ZM-241385 as radioligand
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.28 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359463 | — | — | 1 | 8.96 |
| CHEMBL426053 | — | — | 1 | 8.43 |
| CHEMBL181266 | — | — | 1 | 8.15 |
| CHEMBL367572 | — | — | 1 | 8.14 |
| CHEMBL181267 | — | — | 1 | 8.05 |
| CHEMBL183181 | — | — | 1 | 7.92 |
| CHEMBL183674 | — | — | 1 | 7.92 |
| CHEMBL360136 | — | — | 1 | 7.60 |
| CHEMBL180887 | — | — | 1 | 7.52 |
| CHEMBL182286 | — | — | 1 | 7.48 |
| CHEMBL182486 | — | — | 1 | 7.48 |
| CHEMBL17127 | SCH-58261 | — | 1 | 7.43 |
| CHEMBL183518 | — | — | 1 | 7.43 |
| CHEMBL361819 | — | — | 1 | 7.38 |
| CHEMBL181689 | — | — | 1 | 7.13 |
| CHEMBL2113018 | — | — | 1 | 7.05 |
| CHEMBL180750 | — | — | 1 | 7.04 |
| CHEMBL182612 | — | — | 1 | 6.68 |
| CHEMBL362031 | — | — | 1 | 6.58 |
| CHEMBL179947 | — | — | 1 | 6.55 |
| CHEMBL2113017 | — | — | 1 | 6.51 |
| CHEMBL181268 | — | — | 1 | 6.47 |
| CHEMBL361209 | — | — | 1 | 6.41 |
| CHEMBL2113025 | — | — | 1 | 5.96 |
| CHEMBL360652 | — | — | 1 | 5.80 |
| CHEMBL359678 | — | — | 1 | - |
| CHEMBL360558 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359463 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL426053 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL181266 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL367572 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL181267 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL183181 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL183674 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL360136 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL180887 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL182286 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL182486 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL17127 | SCH-58261 | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL183518 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL361819 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL181689 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL2113018 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL180750 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL182612 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL362031 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL179947 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL2113017 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL181268 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL361209 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL2113025 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL360652 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL359678 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL360558 | — | Ki | > | 500.0 | nM | - |