Assay Detail
Binding
CHEMBL642182
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Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 17 | 5.38 | 6.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL156863 | — | — | 1 | 6.97 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.30 |
| CHEMBL273807 | — | — | 1 | 6.21 |
| CHEMBL69701 | — | — | 1 | 5.87 |
| CHEMBL10873 | — | — | 1 | 5.72 |
| CHEMBL156178 | — | — | 1 | 5.57 |
| CHEMBL63944 | — | — | 1 | 5.50 |
| CHEMBL67110 | — | — | 1 | 5.45 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | — | 1 | 5.37 |
| CHEMBL350469 | — | — | 1 | 5.26 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.17 |
| CHEMBL24107 | — | — | 1 | 5.01 |
| CHEMBL307105 | — | — | 1 | 4.78 |
| CHEMBL36867 | — | — | 1 | 4.76 |
| CHEMBL66610 | — | — | 1 | 4.63 |
| CHEMBL67060 | — | — | 1 | 4.48 |
| CHEMBL304455 | — | — | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL156863 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL273807 | — | Ki | = | 612.0 | nM | 6.21 |
| CHEMBL69701 | — | Ki | = | 1340.0 | nM | 5.87 |
| CHEMBL10873 | — | Ki | = | 1920.0 | nM | 5.72 |
| CHEMBL156178 | — | Ki | = | 2720.0 | nM | 5.57 |
| CHEMBL63944 | — | Ki | = | 3190.0 | nM | 5.50 |
| CHEMBL67110 | — | Ki | = | 3570.0 | nM | 5.45 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | Ki | = | 4230.0 | nM | 5.37 |
| CHEMBL350469 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL24107 | — | Ki | = | 9780.0 | nM | 5.01 |
| CHEMBL307105 | — | Ki | = | 16700.0 | nM | 4.78 |
| CHEMBL36867 | — | Ki | = | 17300.0 | nM | 4.76 |
| CHEMBL66610 | — | Ki | = | 23500.0 | nM | 4.63 |
| CHEMBL67060 | — | Ki | = | 33300.0 | nM | 4.48 |
| CHEMBL304455 | — | Ki | = | 33600.0 | nM | 4.47 |