Assay Detail
Binding
CHEMBL638690
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Binding affinity of specific [3H]R-PIA binding to rat Adenosine A1 receptor in HEK293 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous 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 | 27 | 5.98 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.00 |
| CHEMBL36867 | — | — | 1 | 8.13 |
| CHEMBL37243 | — | — | 1 | 8.12 |
| CHEMBL273807 | — | — | 1 | 7.78 |
| CHEMBL69701 | — | — | 1 | 7.52 |
| CHEMBL36740 | — | — | 1 | 7.41 |
| CHEMBL66337 | — | — | 1 | 7.41 |
| CHEMBL350469 | — | — | 1 | 7.01 |
| CHEMBL156863 | — | — | 1 | 6.66 |
| CHEMBL10873 | — | — | 1 | 6.52 |
| CHEMBL156178 | — | — | 1 | 6.12 |
| CHEMBL63944 | — | — | 1 | 5.78 |
| CHEMBL307105 | — | — | 1 | 5.78 |
| CHEMBL66881 | — | — | 1 | 5.66 |
| CHEMBL302344 | — | — | 1 | 5.25 |
| CHEMBL304455 | — | — | 1 | 5.23 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.16 |
| CHEMBL68278 | — | — | 1 | 5.05 |
| CHEMBL67415 | — | — | 1 | 4.90 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | — | 1 | 4.82 |
| CHEMBL67060 | — | — | 1 | 4.75 |
| CHEMBL67323 | — | — | 1 | 4.63 |
| CHEMBL24107 | — | — | 1 | 4.61 |
| CHEMBL66899 | — | — | 1 | 4.61 |
| CHEMBL67313 | — | — | 1 | 4.61 |
| CHEMBL67228 | — | — | 1 | 4.56 |
| CHEMBL67949 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL36867 | — | Ki | = | 7.46 | nM | 8.13 |
| CHEMBL37243 | — | Ki | = | 7.68 | nM | 8.12 |
| CHEMBL273807 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL69701 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL36740 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL66337 | — | Ki | = | 39.2 | nM | 7.41 |
| CHEMBL350469 | — | Ki | = | 97.7 | nM | 7.01 |
| CHEMBL156863 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL10873 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL156178 | — | Ki | = | 757.0 | nM | 6.12 |
| CHEMBL63944 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL307105 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL66881 | — | Ki | = | 2170.0 | nM | 5.66 |
| CHEMBL302344 | — | Ki | = | 5570.0 | nM | 5.25 |
| CHEMBL304455 | — | Ki | = | 5830.0 | nM | 5.23 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6920.0 | nM | 5.16 |
| CHEMBL68278 | — | Ki | = | 8890.0 | nM | 5.05 |
| CHEMBL67415 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | Ki | = | 15200.0 | nM | 4.82 |
| CHEMBL67060 | — | Ki | = | 17700.0 | nM | 4.75 |
| CHEMBL67323 | — | Ki | = | 23600.0 | nM | 4.63 |
| CHEMBL24107 | — | Ki | = | 24700.0 | nM | 4.61 |
| CHEMBL66899 | — | Ki | = | 24300.0 | nM | 4.61 |
| CHEMBL67313 | — | Ki | = | 24400.0 | nM | 4.61 |
| CHEMBL67228 | — | Ki | = | 27600.0 | nM | 4.56 |
| CHEMBL67949 | — | Ki | = | 37600.0 | nM | 4.42 |