Assay Detail
Binding
CHEMBL640349
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Binding affinity against adenosine A1 receptor of cerebral cortex using [3H]CPX as a radioligand
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 5.04 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29518 | — | — | 1 | 7.22 |
| CHEMBL157655 | — | — | 1 | 6.68 |
| CHEMBL28194 | — | — | 1 | 5.85 |
| CHEMBL29461 | — | — | 1 | 5.77 |
| CHEMBL28075 | — | — | 1 | 5.72 |
| CHEMBL286976 | — | — | 1 | 5.72 |
| CHEMBL288786 | — | — | 1 | 5.68 |
| CHEMBL29272 | — | — | 1 | 5.60 |
| CHEMBL32184 | — | — | 1 | 5.37 |
| CHEMBL28980 | — | — | 1 | 5.22 |
| CHEMBL28879 | — | — | 1 | 5.18 |
| CHEMBL282310 | — | — | 1 | 5.03 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.01 |
| CHEMBL282394 | — | — | 1 | 4.95 |
| CHEMBL28603 | — | — | 1 | 4.94 |
| CHEMBL283454 | — | — | 1 | 4.92 |
| CHEMBL445847 | — | — | 1 | 4.91 |
| CHEMBL28298 | — | — | 1 | 4.91 |
| CHEMBL283412 | — | — | 1 | 4.85 |
| CHEMBL287180 | — | — | 1 | 4.81 |
| CHEMBL32241 | — | — | 1 | 4.80 |
| CHEMBL28559 | — | — | 1 | 4.64 |
| CHEMBL283024 | — | — | 1 | 4.61 |
| CHEMBL31859 | — | — | 1 | 4.52 |
| CHEMBL31838 | — | — | 1 | 4.50 |
| CHEMBL27915 | — | — | 1 | 4.40 |
| CHEMBL283020 | — | — | 1 | 4.38 |
| CHEMBL282160 | — | — | 1 | 4.37 |
| CHEMBL27967 | — | — | 1 | 4.30 |
| CHEMBL279898 | ENPROFYLLINE | 2.0 | 1 | 4.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29518 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL157655 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL28194 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL29461 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL28075 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL286976 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL288786 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL29272 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL32184 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL28980 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL28879 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL282310 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 9800.0 | nM | 5.01 |
| CHEMBL282394 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL28603 | — | Ki | = | 11400.0 | nM | 4.94 |
| CHEMBL283454 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL445847 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL28298 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL283412 | — | Ki | = | 14200.0 | nM | 4.85 |
| CHEMBL287180 | — | Ki | = | 15400.0 | nM | 4.81 |
| CHEMBL32241 | — | Ki | = | 15900.0 | nM | 4.80 |
| CHEMBL28559 | — | Ki | = | 23100.0 | nM | 4.64 |
| CHEMBL283024 | — | Ki | = | 24300.0 | nM | 4.61 |
| CHEMBL31859 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL31838 | — | Ki | = | 31500.0 | nM | 4.50 |
| CHEMBL27915 | — | Ki | = | 39700.0 | nM | 4.40 |
| CHEMBL283020 | — | Ki | = | 41400.0 | nM | 4.38 |
| CHEMBL282160 | — | Ki | = | 43200.0 | nM | 4.37 |
| CHEMBL27967 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL279898 | ENPROFYLLINE | Ki | = | 60700.0 | nM | 4.22 |
| CHEMBL28683 | — | Ki | = | 88600.0 | nM | 4.05 |
| CHEMBL27969 | — | Ki | = | 95700.0 | nM | 4.02 |
| CHEMBL281972 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL29052 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL286741 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL29209 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL28419 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL28300 | — | Ki | = | 112000.0 | nM | - |
| CHEMBL28295 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL27970 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL28684 | — | Ki | > | 200000.0 | nM | - |
| CHEMBL628 | PENTOXIFYLLINE | Ki | = | 180000.0 | nM | - |