Assay Detail
Binding
CHEMBL647247
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Adenosine A2a receptor using [3H]NECA in rat striatal membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.62 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113728 | — | — | 1 | 7.00 |
| CHEMBL294302 | — | — | 1 | 6.08 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 5.96 |
| CHEMBL2113729 | — | — | 1 | 5.26 |
| CHEMBL59466 | — | — | 1 | 5.26 |
| CHEMBL292917 | — | — | 1 | 5.23 |
| CHEMBL59673 | — | — | 1 | 5.21 |
| CHEMBL440115 | FK453 | 1.0 | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113728 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL294302 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2113729 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL59466 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL292917 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL59673 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL440115 | FK453 | IC50 | = | 11000.0 | nM | 4.96 |