Assay Detail
Functional
CHEMBL696391
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 1 uM NECA-stimulated cyclic AMP levels in human platelets
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.43 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307748 | — | — | 1 | 8.10 |
| CHEMBL67026 | — | — | 1 | 8.00 |
| CHEMBL16687 | CGS-15943 | — | 1 | 7.92 |
| CHEMBL17127 | SCH-58261 | — | 1 | 7.92 |
| CHEMBL67994 | — | — | 1 | 7.85 |
| CHEMBL17121 | SCH-63390 | — | 1 | 7.75 |
| CHEMBL69794 | — | — | 1 | 7.70 |
| CHEMBL63520 | — | — | 1 | 7.22 |
| CHEMBL67134 | — | — | 1 | 7.05 |
| CHEMBL416684 | — | — | 1 | 6.83 |
| CHEMBL423852 | — | — | 1 | 6.52 |
| CHEMBL66811 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307748 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL67026 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL16687 | CGS-15943 | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL17127 | SCH-58261 | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL67994 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL17121 | SCH-63390 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL69794 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL63520 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL67134 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL416684 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL423852 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL66811 | — | IC50 | = | 500.0 | nM | 6.30 |