Assay Detail
Binding
CHEMBL641002
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Inhibitory activity against Adenosine A1 Receptor using [3H]CHA in rat cortical membranes
8
Total Activities
8
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
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 | 7.81 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113728 | — | — | 1 | 8.44 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.33 |
| CHEMBL294302 | — | — | 1 | 7.96 |
| CHEMBL59673 | — | — | 1 | 7.82 |
| CHEMBL59466 | — | — | 1 | 7.80 |
| CHEMBL440115 | FK453 | 1.0 | 1 | 7.77 |
| CHEMBL2113729 | — | — | 1 | 7.47 |
| CHEMBL292917 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113728 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL294302 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL59673 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL59466 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL440115 | FK453 | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2113729 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL292917 | — | IC50 | = | 120.0 | nM | 6.92 |