Assay Detail
Binding
CHEMBL641304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-SCH- 58261 from Adenosine A2A receptor in rat striatal membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| 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 | 13 | 7.04 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423542 | — | — | 1 | 9.23 |
| CHEMBL16867 | — | — | 1 | 9.15 |
| CHEMBL88147 | — | — | 1 | 7.99 |
| CHEMBL137879 | — | — | 1 | 7.95 |
| CHEMBL344706 | — | — | 1 | 7.69 |
| CHEMBL422820 | — | — | 1 | 5.85 |
| CHEMBL137950 | — | — | 1 | 5.77 |
| CHEMBL302765 | — | — | 1 | 5.70 |
| CHEMBL141154 | — | — | 1 | 5.55 |
| CHEMBL342906 | — | — | 1 | 5.50 |
| CHEMBL138332 | — | — | 1 | - |
| CHEMBL139182 | — | — | 1 | - |
| CHEMBL65271 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423542 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL16867 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL88147 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL137879 | — | Ki | = | 11.15 | nM | 7.95 |
| CHEMBL344706 | — | Ki | = | 20.23 | nM | 7.69 |
| CHEMBL422820 | — | Ki | = | 1398.0 | nM | 5.85 |
| CHEMBL137950 | — | Ki | = | 1698.0 | nM | 5.77 |
| CHEMBL302765 | — | Ki | = | 1993.0 | nM | 5.70 |
| CHEMBL141154 | — | Ki | = | 2799.0 | nM | 5.55 |
| CHEMBL342906 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL138332 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL139182 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL65271 | — | Ki | > | 10000.0 | nM | - |