Assay Detail
Binding
CHEMBL642257
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.66 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL464859 | NECA | — | 1 | 7.85 |
| CHEMBL112756 | — | — | 1 | 7.75 |
| CHEMBL7909 | — | — | 1 | 7.20 |
| CHEMBL113476 | — | — | 1 | 7.11 |
| CHEMBL7113 | — | — | 1 | 7.07 |
| CHEMBL7953 | — | — | 1 | 6.92 |
| CHEMBL110979 | — | — | 1 | 6.69 |
| CHEMBL7142 | — | — | 1 | 6.63 |
| CHEMBL7327 | — | — | 1 | 6.60 |
| CHEMBL7608 | — | — | 1 | 6.58 |
| CHEMBL326752 | — | — | 1 | 6.56 |
| CHEMBL269112 | — | — | 1 | 6.53 |
| CHEMBL324100 | — | — | 1 | 6.50 |
| CHEMBL109691 | — | — | 1 | 6.46 |
| CHEMBL109494 | — | — | 1 | 6.35 |
| CHEMBL109687 | — | — | 1 | 6.34 |
| CHEMBL7334 | — | — | 1 | 6.33 |
| CHEMBL7098 | — | — | 1 | 6.09 |
| CHEMBL307199 | — | — | 1 | 6.05 |
| CHEMBL113518 | — | — | 1 | 6.00 |
| CHEMBL273657 | — | — | 1 | 5.75 |
| CHEMBL7493 | — | — | 1 | 5.69 |
| CHEMBL7269 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL464859 | NECA | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL112756 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL7909 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL113476 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL7113 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL7953 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL110979 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL7142 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL7327 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL7608 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL326752 | — | Ki | = | 274.0 | nM | 6.56 |
| CHEMBL269112 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL324100 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL109691 | — | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL109494 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL109687 | — | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL7334 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL7098 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL307199 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL113518 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL273657 | — | Ki | = | 1780.0 | nM | 5.75 |
| CHEMBL7493 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL7269 | — | Ki | = | 3900.0 | nM | 5.41 |