Assay Detail
Binding
CHEMBL860036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CHA from adenosine A1 receptor in bovine cerebral cortical membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.24 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL8966 | — | — | 1 | 8.30 |
| CHEMBL200835 | — | — | 1 | 7.30 |
| CHEMBL200479 | — | — | 1 | 6.82 |
| CHEMBL197333 | — | — | 1 | 6.57 |
| CHEMBL371697 | — | — | 1 | 6.29 |
| CHEMBL197325 | — | — | 1 | 6.28 |
| CHEMBL334286 | — | — | 1 | 6.24 |
| CHEMBL97286 | — | — | 1 | 6.00 |
| CHEMBL98678 | — | — | 1 | 5.97 |
| CHEMBL200687 | — | — | 1 | 5.97 |
| CHEMBL330399 | — | — | 1 | 5.95 |
| CHEMBL197376 | — | — | 1 | 5.84 |
| CHEMBL327853 | — | — | 1 | 5.71 |
| CHEMBL198574 | — | — | 1 | 5.62 |
| CHEMBL328437 | — | — | 1 | 5.53 |
| CHEMBL325715 | — | — | 1 | 5.49 |
| CHEMBL316824 | — | — | 1 | 5.44 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.42 |
| CHEMBL8907 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL8966 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL200835 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL200479 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL197333 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL371697 | — | Ki | = | 508.0 | nM | 6.29 |
| CHEMBL197325 | — | Ki | = | 525.0 | nM | 6.28 |
| CHEMBL334286 | — | Ki | = | 578.0 | nM | 6.24 |
| CHEMBL97286 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL98678 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL200687 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL330399 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL197376 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL327853 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL198574 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL328437 | — | Ki | = | 2940.0 | nM | 5.53 |
| CHEMBL325715 | — | Ki | = | 3220.0 | nM | 5.49 |
| CHEMBL316824 | — | Ki | = | 3660.0 | nM | 5.44 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL8907 | — | Ki | = | 14170.0 | nM | 4.85 |