Assay Detail
Binding
CHEMBL649770
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Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.63 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273807 | — | — | 1 | 7.89 |
| CHEMBL10873 | — | — | 1 | 6.76 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.73 |
| CHEMBL67110 | — | — | 1 | 5.77 |
| CHEMBL39986 | — | — | 1 | 5.73 |
| CHEMBL304455 | — | — | 1 | 5.67 |
| CHEMBL307105 | — | — | 1 | 5.47 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | — | 1 | 5.27 |
| CHEMBL67228 | — | — | 1 | 5.26 |
| CHEMBL63944 | — | — | 1 | 4.99 |
| CHEMBL67323 | — | — | 1 | 4.85 |
| CHEMBL67313 | — | — | 1 | 4.82 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.82 |
| CHEMBL67060 | — | — | 1 | 4.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273807 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL10873 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL67110 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL39986 | — | Ki | = | 1880.0 | nM | 5.73 |
| CHEMBL304455 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL307105 | — | Ki | = | 3360.0 | nM | 5.47 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | Ki | = | 5390.0 | nM | 5.27 |
| CHEMBL67228 | — | Ki | = | 5530.0 | nM | 5.26 |
| CHEMBL63944 | — | Ki | = | 10200.0 | nM | 4.99 |
| CHEMBL67323 | — | Ki | = | 14200.0 | nM | 4.85 |
| CHEMBL67313 | — | Ki | = | 15300.0 | nM | 4.82 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 15100.0 | nM | 4.82 |
| CHEMBL67060 | — | Ki | = | 18700.0 | nM | 4.73 |