Assay Detail
Binding
CHEMBL2034748
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.79 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2030706 | — | — | 1 | 7.80 |
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL7608 | — | — | 1 | 7.48 |
| CHEMBL2030704 | — | — | 1 | 7.30 |
| CHEMBL113518 | — | — | 1 | 6.81 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.47 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.40 |
| CHEMBL7098 | — | — | 1 | 5.58 |
| CHEMBL324100 | — | — | 1 | 5.49 |
| CHEMBL7113 | — | — | 1 | - |
| CHEMBL7909 | — | — | 1 | - |
| CHEMBL112756 | — | — | 1 | - |
| CHEMBL2030703 | — | — | 1 | - |
| CHEMBL326752 | — | — | 1 | - |
| CHEMBL2030705 | — | — | 1 | - |
| CHEMBL2030707 | — | — | 1 | - |
| CHEMBL2030708 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2030706 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL7608 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL2030704 | — | Ki | = | 50.6 | nM | 7.30 |
| CHEMBL113518 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL7098 | — | Ki | = | 2608.0 | nM | 5.58 |
| CHEMBL324100 | — | Ki | = | 3277.0 | nM | 5.49 |
| CHEMBL7113 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL7909 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL112756 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2030703 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL326752 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2030705 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2030707 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2030708 | — | Ki | > | 10000.0 | nM | - |