Assay Detail
Binding
CHEMBL640787
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Antagonism of binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptors on rat cortical membranes
24
Total Activities
24
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
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.09 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273671 | — | — | 1 | 8.60 |
| CHEMBL27155 | — | — | 1 | 8.54 |
| CHEMBL158507 | — | — | 1 | 7.89 |
| CHEMBL27047 | — | — | 1 | 7.30 |
| CHEMBL423239 | — | — | 1 | 6.77 |
| CHEMBL418333 | — | — | 1 | 6.68 |
| CHEMBL276830 | — | — | 1 | 6.64 |
| CHEMBL11054 | — | — | 1 | 6.47 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.40 |
| CHEMBL157655 | — | — | 1 | 6.16 |
| CHEMBL415248 | — | — | 1 | 6.12 |
| CHEMBL11120 | — | — | 1 | 6.07 |
| CHEMBL11033 | — | — | 1 | 5.96 |
| CHEMBL20402 | — | — | 1 | 5.75 |
| CHEMBL11048 | — | — | 1 | 5.52 |
| CHEMBL279688 | — | — | 1 | 5.46 |
| CHEMBL8488 | — | — | 1 | 5.35 |
| CHEMBL89062 | — | — | 1 | 5.19 |
| CHEMBL20613 | — | — | 1 | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.85 |
| CHEMBL21053 | — | — | 1 | 4.77 |
| CHEMBL273953 | — | — | 1 | 4.50 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.26 |
| CHEMBL11146 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273671 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL27155 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL158507 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL27047 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL423239 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL418333 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL276830 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL11054 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL157655 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL415248 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL11120 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL11033 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL20402 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL11048 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL279688 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL8488 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL89062 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL20613 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL21053 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL273953 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL113 | CAFFEINE | Ki | = | 55000.0 | nM | 4.26 |
| CHEMBL11146 | — | Ki | > | 50000.0 | nM | - |