Assay Detail
Binding
CHEMBL642190
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Displacement of [3H]DPCPX from Adenosine A1 receptor of rat brain 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 | 6.68 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16867 | — | — | 1 | 8.67 |
| CHEMBL423542 | — | — | 1 | 7.95 |
| CHEMBL88147 | — | — | 1 | 7.28 |
| CHEMBL137879 | — | — | 1 | 7.02 |
| CHEMBL344706 | — | — | 1 | 6.86 |
| CHEMBL137950 | — | — | 1 | 5.98 |
| CHEMBL422820 | — | — | 1 | 5.89 |
| CHEMBL139182 | — | — | 1 | 5.82 |
| CHEMBL138332 | — | — | 1 | 5.80 |
| CHEMBL141154 | — | — | 1 | 5.57 |
| CHEMBL302765 | — | — | 1 | - |
| CHEMBL342906 | — | — | 1 | - |
| CHEMBL65271 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16867 | — | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL423542 | — | Ki | = | 11.13 | nM | 7.95 |
| CHEMBL88147 | — | Ki | = | 52.7 | nM | 7.28 |
| CHEMBL137879 | — | Ki | = | 95.09 | nM | 7.02 |
| CHEMBL344706 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL137950 | — | Ki | = | 1049.0 | nM | 5.98 |
| CHEMBL422820 | — | Ki | = | 1282.0 | nM | 5.89 |
| CHEMBL139182 | — | Ki | = | 1514.0 | nM | 5.82 |
| CHEMBL138332 | — | Ki | = | 1582.0 | nM | 5.80 |
| CHEMBL141154 | — | Ki | = | 2699.0 | nM | 5.57 |
| CHEMBL302765 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL342906 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL65271 | — | Ki | > | 10000.0 | nM | - |