Assay Detail
Binding
CHEMBL649882
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A2 receptor in rat striatum by the displacement of [3H]N-ethyladenosine-5''-uronamide(NECA).
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.57 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34504 | — | — | 1 | 7.41 |
| CHEMBL33795 | — | — | 1 | 7.33 |
| CHEMBL34120 | — | — | 1 | 7.24 |
| CHEMBL27155 | — | — | 1 | 7.22 |
| CHEMBL34789 | — | — | 1 | 7.09 |
| CHEMBL283908 | — | — | 1 | 7.07 |
| CHEMBL18887 | — | — | 1 | 7.03 |
| CHEMBL158507 | — | — | 1 | 6.94 |
| CHEMBL33816 | — | — | 1 | 6.87 |
| CHEMBL33673 | — | — | 1 | 6.72 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.64 |
| CHEMBL34004 | — | — | 1 | 6.61 |
| CHEMBL33611 | — | — | 1 | 6.59 |
| CHEMBL32253 | — | — | 1 | 6.58 |
| CHEMBL160369 | — | — | 1 | 6.50 |
| CHEMBL285865 | — | — | 1 | 6.48 |
| CHEMBL416585 | — | — | 1 | 6.39 |
| CHEMBL34784 | — | — | 1 | 6.35 |
| CHEMBL33762 | — | — | 1 | 6.32 |
| CHEMBL428341 | — | — | 1 | 6.26 |
| CHEMBL33115 | — | — | 1 | 6.23 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.19 |
| CHEMBL284578 | — | — | 1 | 6.00 |
| CHEMBL285074 | — | — | 1 | 6.00 |
| CHEMBL287011 | — | — | 1 | 5.98 |
| CHEMBL32963 | — | — | 1 | 5.84 |
| CHEMBL284825 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34504 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL33795 | — | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL34120 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL27155 | — | Ki | = | 60.8 | nM | 7.22 |
| CHEMBL34789 | — | Ki | = | 81.5 | nM | 7.09 |
| CHEMBL283908 | — | Ki | = | 85.1 | nM | 7.07 |
| CHEMBL18887 | — | Ki | = | 93.3 | nM | 7.03 |
| CHEMBL158507 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL33816 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL33673 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL34004 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL33611 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL32253 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL160369 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL285865 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL416585 | — | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL34784 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL33762 | — | Ki | = | 476.0 | nM | 6.32 |
| CHEMBL428341 | — | Ki | = | 553.0 | nM | 6.26 |
| CHEMBL33115 | — | Ki | = | 593.0 | nM | 6.23 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 644.0 | nM | 6.19 |
| CHEMBL284578 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL285074 | — | Ki | = | 995.0 | nM | 6.00 |
| CHEMBL287011 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL32963 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL284825 | — | Ki | = | 3760.0 | nM | 5.42 |