Assay Detail
Binding
CHEMBL955677
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Displacement of [125I]DPCPX from adenosine A1 receptor in bovine brain membrane
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.98 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL508203 | — | — | 1 | 8.39 |
| CHEMBL484313 | — | — | 1 | 8.34 |
| CHEMBL484112 | — | — | 1 | 7.68 |
| CHEMBL519319 | — | — | 1 | 7.44 |
| CHEMBL484720 | — | — | 1 | 7.26 |
| CHEMBL502005 | — | — | 1 | 7.24 |
| CHEMBL16488 | — | — | 1 | 7.05 |
| CHEMBL484314 | — | — | 1 | 7.00 |
| CHEMBL521299 | — | — | 1 | 6.97 |
| CHEMBL482504 | — | — | 1 | 6.80 |
| CHEMBL483310 | — | — | 1 | 6.79 |
| CHEMBL483309 | — | — | 1 | 6.68 |
| CHEMBL526134 | — | — | 1 | 6.63 |
| CHEMBL484520 | — | — | 1 | 6.45 |
| CHEMBL484497 | — | — | 1 | 6.33 |
| CHEMBL483116 | — | — | 1 | 5.55 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.42 |
| CHEMBL482701 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL508203 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL484313 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL484112 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL519319 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL484720 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL502005 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL16488 | — | Ki | = | 89.6 | nM | 7.05 |
| CHEMBL484314 | — | Ki | = | 100.6 | nM | 7.00 |
| CHEMBL521299 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL482504 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL483310 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL483309 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL526134 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL484520 | — | Ki | = | 359.0 | nM | 6.45 |
| CHEMBL484497 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL483116 | — | Ki | = | 2840.0 | nM | 5.55 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL482701 | — | Ki | = | 4700.0 | nM | 5.33 |