Assay Detail
Binding
CHEMBL4012871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A2A Receptor Subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 6.98 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL487754 | — | — | 1 | 8.92 |
| CHEMBL464859 | NECA | — | 1 | 8.34 |
| CHEMBL4089735 | — | — | 1 | 8.09 |
| CHEMBL4066559 | — | — | 1 | 8.05 |
| CHEMBL4080925 | — | — | 1 | 7.89 |
| CHEMBL4068548 | — | — | 1 | 7.85 |
| CHEMBL4070286 | — | — | 1 | 7.75 |
| CHEMBL4088805 | — | — | 1 | 7.70 |
| CHEMBL4097391 | — | — | 1 | 7.36 |
| CHEMBL4081800 | — | — | 1 | 7.35 |
| CHEMBL4059885 | — | — | 1 | 7.35 |
| CHEMBL4094093 | — | — | 1 | 7.33 |
| CHEMBL4105169 | — | — | 1 | 7.17 |
| CHEMBL4082584 | — | — | 1 | 6.89 |
| CHEMBL4090423 | — | — | 1 | 6.61 |
| CHEMBL4061617 | — | — | 1 | 6.61 |
| CHEMBL4082891 | — | — | 1 | 6.21 |
| CHEMBL4059695 | — | — | 1 | 6.16 |
| CHEMBL4097464 | — | — | 1 | 6.00 |
| CHEMBL4062442 | — | — | 1 | 5.83 |
| CHEMBL4067571 | — | — | 1 | 5.76 |
| CHEMBL4072104 | — | — | 1 | 5.67 |
| CHEMBL4086268 | — | — | 1 | 5.43 |
| CHEMBL4100596 | — | — | 1 | 5.24 |
| CHEMBL4079325 | — | — | 1 | - |
| CHEMBL4069525 | — | — | 1 | - |
| CHEMBL4098254 | — | — | 1 | - |
| CHEMBL4080233 | — | — | 1 | - |
| CHEMBL4081637 | — | — | 1 | - |
| CHEMBL4098141 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL487754 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL464859 | NECA | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL4089735 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL4066559 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL4080925 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4068548 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4070286 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4088805 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4097391 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL4081800 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4059885 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4094093 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL4105169 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL4082584 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL4061617 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL4090423 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL4082891 | — | Ki | = | 616.0 | nM | 6.21 |
| CHEMBL4059695 | — | Ki | = | 698.0 | nM | 6.16 |
| CHEMBL4097464 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4062442 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL4067571 | — | Ki | = | 1743.0 | nM | 5.76 |
| CHEMBL4072104 | — | Ki | = | 2142.0 | nM | 5.67 |
| CHEMBL4086268 | — | Ki | = | 3704.0 | nM | 5.43 |
| CHEMBL4100596 | — | Ki | = | 5740.0 | nM | 5.24 |
| CHEMBL4064795 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4098310 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4071262 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4092862 | — | Ki | - | — | - | |
| CHEMBL4090541 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4089671 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4079360 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4103595 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4095840 | — | Ki | - | — | - | |
| CHEMBL4068501 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4071082 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4088110 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4059837 | — | Ki | - | — | - | |
| CHEMBL4098141 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4081637 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4080233 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4098254 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4069525 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4079325 | — | Ki | > | 30000.0 | nM | - |