Assay Detail
Binding
CHEMBL644670
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Displacement of specific [3H]-SCH- 58261 binding at human Adenosine A2A receptor expressed in HEK293 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.67 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423542 | — | — | 1 | 9.74 |
| CHEMBL16867 | — | — | 1 | 9.51 |
| CHEMBL137879 | — | — | 1 | 8.72 |
| CHEMBL344706 | — | — | 1 | 8.59 |
| CHEMBL137950 | — | — | 1 | 6.96 |
| CHEMBL422820 | — | — | 1 | 6.91 |
| CHEMBL302765 | — | — | 1 | 6.85 |
| CHEMBL141154 | — | — | 1 | 6.73 |
| CHEMBL342906 | — | — | 1 | 6.70 |
| CHEMBL139182 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423542 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL16867 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL137879 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL344706 | — | Ki | = | 2.55 | nM | 8.59 |
| CHEMBL137950 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL422820 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL302765 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL141154 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL342906 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL139182 | — | Ki | = | 1015.0 | nM | 5.99 |