Assay Detail
Binding
CHEMBL640429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane
32
Total Activities
32
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 of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 5.84 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325948 | — | — | 1 | 8.14 |
| CHEMBL26138 | — | — | 1 | 8.04 |
| CHEMBL114886 | — | — | 1 | 8.00 |
| CHEMBL25976 | — | — | 1 | 7.89 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.20 |
| CHEMBL112669 | — | — | 1 | 6.80 |
| CHEMBL294463 | — | — | 1 | 6.65 |
| CHEMBL419403 | — | — | 1 | 6.60 |
| CHEMBL114975 | — | — | 1 | 6.48 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL114760 | — | — | 1 | 6.34 |
| CHEMBL423239 | — | — | 1 | 6.20 |
| CHEMBL355370 | — | — | 1 | 6.16 |
| CHEMBL418333 | — | — | 1 | 6.10 |
| CHEMBL16997 | — | — | 1 | 6.10 |
| CHEMBL17123 | — | — | 1 | 6.06 |
| CHEMBL320786 | — | — | 1 | 5.92 |
| CHEMBL27041 | — | — | 1 | 5.66 |
| CHEMBL16724 | — | — | 1 | 5.37 |
| CHEMBL333143 | — | — | 1 | 5.23 |
| CHEMBL112034 | — | — | 1 | 5.04 |
| CHEMBL113986 | — | — | 1 | 4.78 |
| CHEMBL116874 | — | — | 1 | 4.70 |
| CHEMBL327016 | — | — | 1 | 4.63 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.60 |
| CHEMBL114770 | — | — | 1 | 4.53 |
| CHEMBL92364 | — | — | 1 | 4.38 |
| CHEMBL24759 | — | — | 1 | 4.34 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.32 |
| CHEMBL114745 | — | — | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325948 | — | Ki | = | 7.22 | nM | 8.14 |
| CHEMBL26138 | — | Ki | = | 9.08 | nM | 8.04 |
| CHEMBL114886 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL25976 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL112669 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL294463 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL419403 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL114975 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL114760 | — | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL423239 | — | Ki | = | 637.0 | nM | 6.20 |
| CHEMBL355370 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL418333 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL16997 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL17123 | — | Ki | = | 874.0 | nM | 6.06 |
| CHEMBL320786 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL27041 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL16724 | — | Ki | = | 4290.0 | nM | 5.37 |
| CHEMBL333143 | — | Ki | = | 5850.0 | nM | 5.23 |
| CHEMBL112034 | — | Ki | = | 9220.0 | nM | 5.04 |
| CHEMBL113986 | — | Ki | = | 16500.0 | nM | 4.78 |
| CHEMBL116874 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL327016 | — | Ki | = | 23200.0 | nM | 4.63 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL114770 | — | Ki | = | 29300.0 | nM | 4.53 |
| CHEMBL92364 | — | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL24759 | — | Ki | = | 46000.0 | nM | 4.34 |
| CHEMBL113 | CAFFEINE | Ki | = | 48000.0 | nM | 4.32 |
| CHEMBL114745 | — | Ki | = | 67800.0 | nM | 4.17 |
| CHEMBL115608 | — | Ki | = | 71700.0 | nM | 4.14 |
| CHEMBL324036 | — | Ki | = | 113000.0 | nM | - |