Assay Detail
Binding
CHEMBL946044
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Displacement of [3H]-CPX from human A1 receptor expressed in CHO cell membranes
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 5.96 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254725 | — | — | 1 | 7.12 |
| CHEMBL251870 | — | — | 1 | 6.80 |
| CHEMBL251869 | — | — | 1 | 6.77 |
| CHEMBL253252 | — | — | 1 | 6.68 |
| CHEMBL252045 | — | — | 1 | 6.00 |
| CHEMBL427887 | — | — | 1 | 5.85 |
| CHEMBL252245 | — | — | 1 | 5.82 |
| CHEMBL404130 | — | — | 1 | 5.80 |
| CHEMBL404131 | — | — | 1 | 5.75 |
| CHEMBL252069 | — | — | 1 | 5.48 |
| CHEMBL251854 | — | — | 1 | 5.46 |
| CHEMBL253048 | — | — | 1 | 5.38 |
| CHEMBL251874 | — | — | 1 | 5.29 |
| CHEMBL251873 | — | — | 1 | 5.25 |
| CHEMBL251871 | — | — | 1 | - |
| CHEMBL404129 | — | — | 1 | - |
| CHEMBL427713 | — | — | 1 | - |
| CHEMBL251872 | — | — | 1 | - |
| CHEMBL430023 | — | — | 1 | - |
| CHEMBL252070 | — | — | 1 | - |
| CHEMBL402651 | — | — | 1 | - |
| CHEMBL251875 | — | — | 1 | - |
| CHEMBL252068 | — | — | 1 | - |
| CHEMBL404349 | — | — | 1 | - |
| CHEMBL401834 | — | — | 1 | - |
| CHEMBL404348 | — | — | 1 | - |
| CHEMBL442434 | — | — | 1 | - |
| CHEMBL253049 | — | — | 1 | - |
| CHEMBL404168 | — | — | 1 | - |
| CHEMBL251876 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254725 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL251870 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL251869 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL253252 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL252045 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL427887 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL252245 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL404130 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL404131 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL252069 | — | Ki | = | 3290.0 | nM | 5.48 |
| CHEMBL251854 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL253048 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL251874 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL251873 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL251878 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL252074 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL403975 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL252272 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL251879 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL251880 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL251881 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL252048 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL251871 | — | Ki | - | — | - | |
| CHEMBL404129 | — | Ki | - | — | - | |
| CHEMBL427713 | — | Ki | - | — | - | |
| CHEMBL251872 | — | Ki | - | — | - | |
| CHEMBL430023 | — | Ki | - | — | - | |
| CHEMBL252070 | — | Ki | - | — | - | |
| CHEMBL402651 | — | Ki | - | — | - | |
| CHEMBL251875 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL252068 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL404349 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL401834 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL404348 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL442434 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL253049 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL404168 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL251876 | — | Ki | > | 6000.0 | nM | - |