Assay Detail
Binding
CHEMBL640345
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Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 5.21 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446679 | — | — | 1 | 7.70 |
| CHEMBL157655 | — | — | 1 | 6.70 |
| CHEMBL28194 | — | — | 1 | 5.85 |
| CHEMBL130969 | — | — | 1 | 5.72 |
| CHEMBL286976 | — | — | 1 | 5.72 |
| CHEMBL68278 | — | — | 1 | 5.52 |
| CHEMBL39986 | — | — | 1 | 5.48 |
| CHEMBL112369 | — | — | 1 | 5.47 |
| CHEMBL130503 | — | — | 1 | 5.37 |
| CHEMBL132001 | — | — | 1 | 5.22 |
| CHEMBL131275 | — | — | 1 | 5.14 |
| CHEMBL334813 | — | — | 1 | 5.12 |
| CHEMBL278332 | — | — | 1 | 5.11 |
| CHEMBL282310 | — | — | 1 | 5.03 |
| CHEMBL127167 | — | — | 1 | 5.01 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.01 |
| CHEMBL24107 | — | — | 1 | 5.01 |
| CHEMBL1250 | 1-METHYLXANTHINE | — | 1 | 4.94 |
| CHEMBL132052 | — | — | 1 | 4.93 |
| CHEMBL131164 | — | — | 1 | 4.92 |
| CHEMBL283412 | — | — | 1 | 4.85 |
| CHEMBL417654 | — | — | 1 | 4.84 |
| CHEMBL128900 | — | — | 1 | 4.74 |
| CHEMBL334849 | — | — | 1 | 4.67 |
| CHEMBL337001 | — | — | 1 | 4.39 |
| CHEMBL279898 | ENPROFYLLINE | 2.0 | 1 | 4.22 |
| CHEMBL131371 | — | — | 1 | 4.04 |
| CHEMBL131181 | — | — | 1 | - |
| CHEMBL1424 | XANTHINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446679 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL157655 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL28194 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL130969 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL286976 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL68278 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL39986 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL112369 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL130503 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL132001 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL131275 | — | Ki | = | 7300.0 | nM | 5.14 |
| CHEMBL334813 | — | Ki | = | 7600.0 | nM | 5.12 |
| CHEMBL278332 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL282310 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL127167 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL24107 | — | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL1250 | 1-METHYLXANTHINE | Ki | = | 11500.0 | nM | 4.94 |
| CHEMBL132052 | — | Ki | = | 11800.0 | nM | 4.93 |
| CHEMBL131164 | — | Ki | = | 12100.0 | nM | 4.92 |
| CHEMBL283412 | — | Ki | = | 14200.0 | nM | 4.85 |
| CHEMBL417654 | — | Ki | = | 14500.0 | nM | 4.84 |
| CHEMBL128900 | — | Ki | = | 18200.0 | nM | 4.74 |
| CHEMBL334849 | — | Ki | = | 21400.0 | nM | 4.67 |
| CHEMBL337001 | — | Ki | = | 40400.0 | nM | 4.39 |
| CHEMBL279898 | ENPROFYLLINE | Ki | = | 60700.0 | nM | 4.22 |
| CHEMBL131371 | — | Ki | = | 90600.0 | nM | 4.04 |
| CHEMBL131181 | — | Ki | = | 117000.0 | nM | - |
| CHEMBL1424 | XANTHINE | Ki | > | 200000.0 | nM | - |