Assay Detail
Binding
CHEMBL640472
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Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.03 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.82 |
| CHEMBL278906 | — | — | 1 | 8.48 |
| CHEMBL16867 | — | — | 1 | 8.33 |
| CHEMBL315150 | — | — | 1 | 8.25 |
| CHEMBL16687 | CGS-15943 | — | 1 | 8.19 |
| CHEMBL16894 | — | — | 1 | 7.52 |
| CHEMBL440458 | — | — | 1 | 6.94 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.92 |
| CHEMBL16509 | — | — | 1 | 6.92 |
| CHEMBL17302 | — | — | 1 | 6.72 |
| CHEMBL276738 | — | — | 1 | 6.68 |
| CHEMBL17094 | — | — | 1 | 6.63 |
| CHEMBL16692 | — | — | 1 | 6.48 |
| CHEMBL280067 | — | — | 1 | 6.37 |
| CHEMBL275636 | — | — | 1 | 6.33 |
| CHEMBL17121 | SCH-63390 | — | 1 | 6.30 |
| CHEMBL277589 | — | — | 1 | 6.19 |
| CHEMBL16508 | — | — | 1 | 6.01 |
| CHEMBL273590 | — | — | 1 | 5.57 |
| CHEMBL17013 | — | — | 1 | - |
| CHEMBL17281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL278906 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL16867 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL315150 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL16687 | CGS-15943 | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL16894 | — | Ki | = | 30.4 | nM | 7.52 |
| CHEMBL440458 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL17127 | SCH-58261 | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL16509 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL17302 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL276738 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL17094 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL16692 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL280067 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL275636 | — | Ki | = | 471.0 | nM | 6.33 |
| CHEMBL17121 | SCH-63390 | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL277589 | — | Ki | = | 651.0 | nM | 6.19 |
| CHEMBL16508 | — | Ki | = | 978.0 | nM | 6.01 |
| CHEMBL273590 | — | Ki | = | 2705.0 | nM | 5.57 |
| CHEMBL17013 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL17281 | — | Ki | > | 1000.0 | nM | - |