Assay Detail
Binding
CHEMBL642857
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Antagonism of adenosine A1 receptor assessed from the ability to inhibit binding of [3H]cyclohexyladenosine to rat cerebral cortical membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Mesoionic xanthine analogues: antagonists of adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 4.60 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.10 |
| CHEMBL157655 | — | — | 1 | 5.82 |
| CHEMBL416013 | — | — | 1 | 5.19 |
| CHEMBL24774 | — | — | 1 | 5.16 |
| CHEMBL285357 | — | — | 1 | 4.70 |
| CHEMBL285334 | — | — | 1 | 4.57 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.55 |
| CHEMBL29541 | — | — | 1 | 4.52 |
| CHEMBL29416 | — | — | 1 | 4.43 |
| CHEMBL282776 | — | — | 1 | 4.39 |
| CHEMBL29590 | — | — | 1 | 4.35 |
| CHEMBL29534 | — | — | 1 | 4.27 |
| CHEMBL282126 | — | — | 1 | 4.24 |
| CHEMBL29471 | — | — | 1 | 4.22 |
| CHEMBL29782 | — | — | 1 | 4.14 |
| CHEMBL30026 | — | — | 1 | 4.10 |
| CHEMBL28939 | — | — | 1 | 4.02 |
| CHEMBL30057 | — | — | 1 | 4.00 |
| CHEMBL30259 | — | — | 1 | - |
| CHEMBL283189 | — | — | 1 | - |
| CHEMBL28135 | — | — | 1 | - |
| CHEMBL29526 | — | — | 1 | - |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | - |
| CHEMBL29478 | — | — | 1 | - |
| CHEMBL283269 | — | — | 1 | - |
| CHEMBL29241 | — | — | 1 | - |
| CHEMBL281103 | — | — | 1 | - |
| CHEMBL29229 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL157655 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL416013 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL24774 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL285357 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL285334 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL29541 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL29416 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL282776 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL29590 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL29534 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL282126 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL29471 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL29782 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL30026 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL28939 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL30057 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL30259 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL283189 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL28135 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL29526 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL113 | CAFFEINE | IC50 | = | 110000.0 | nM | - |
| CHEMBL29478 | — | IC50 | = | 160000.0 | nM | - |
| CHEMBL283269 | — | IC50 | = | 160000.0 | nM | - |
| CHEMBL29241 | — | IC50 | = | 290000.0 | nM | - |
| CHEMBL281103 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL29229 | — | IC50 | = | 110000.0 | nM | - |