Assay Detail
Binding
CHEMBL4012872
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NECA from human adenosine receptor A2A 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 | 7.00 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4064795 | — | — | 1 | 8.54 |
| CHEMBL4068548 | — | — | 1 | 8.46 |
| CHEMBL4059885 | — | — | 1 | 8.29 |
| CHEMBL4097391 | — | — | 1 | 8.17 |
| CHEMBL4079360 | — | — | 1 | 8.14 |
| CHEMBL4079325 | — | — | 1 | 8.13 |
| CHEMBL4080925 | — | — | 1 | 8.00 |
| CHEMBL4071262 | — | — | 1 | 7.97 |
| CHEMBL464859 | NECA | — | 1 | 7.80 |
| CHEMBL4081800 | — | — | 1 | 7.35 |
| CHEMBL4088805 | — | — | 1 | 7.11 |
| CHEMBL4070286 | — | — | 1 | 6.86 |
| CHEMBL4094093 | — | — | 1 | 6.63 |
| CHEMBL4061617 | — | — | 1 | 6.51 |
| CHEMBL4082584 | — | — | 1 | 6.41 |
| CHEMBL4089735 | — | — | 1 | 6.40 |
| CHEMBL4090423 | — | — | 1 | 6.38 |
| CHEMBL4105169 | — | — | 1 | 6.31 |
| CHEMBL4086268 | — | — | 1 | 6.15 |
| CHEMBL4067571 | — | — | 1 | 5.98 |
| CHEMBL4097464 | — | — | 1 | 5.88 |
| CHEMBL487754 | — | — | 1 | 5.69 |
| CHEMBL4066559 | — | — | 1 | 5.46 |
| CHEMBL4059695 | — | — | 1 | 5.39 |
| CHEMBL4071082 | — | — | 1 | - |
| CHEMBL4082891 | — | — | 1 | - |
| CHEMBL4089671 | — | — | 1 | - |
| CHEMBL4081637 | — | — | 1 | - |
| CHEMBL4098141 | — | — | 1 | - |
| CHEMBL4098310 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4064795 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4068548 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL4059885 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL4097391 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL4079360 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL4079325 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL4080925 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4071262 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL464859 | NECA | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4081800 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4088805 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4070286 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL4094093 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL4061617 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL4082584 | — | Ki | = | 387.0 | nM | 6.41 |
| CHEMBL4089735 | — | Ki | = | 402.0 | nM | 6.40 |
| CHEMBL4090423 | — | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL4105169 | — | Ki | = | 485.0 | nM | 6.31 |
| CHEMBL4086268 | — | Ki | = | 708.0 | nM | 6.15 |
| CHEMBL4067571 | — | Ki | = | 1038.0 | nM | 5.98 |
| CHEMBL4097464 | — | Ki | = | 1319.0 | nM | 5.88 |
| CHEMBL487754 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL4066559 | — | Ki | = | 3480.0 | nM | 5.46 |
| CHEMBL4059695 | — | Ki | = | 4066.0 | nM | 5.39 |
| CHEMBL4100596 | — | Ki | - | — | - | |
| CHEMBL4072104 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4092862 | — | Ki | - | — | - | |
| CHEMBL4090541 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4069525 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4098254 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4080233 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4059837 | — | Ki | - | — | - | |
| CHEMBL4088110 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4068501 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4095840 | — | Ki | - | — | - | |
| CHEMBL4062442 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4103595 | — | Ki | - | — | - | |
| CHEMBL4098310 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4098141 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4081637 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4089671 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4082891 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL4071082 | — | Ki | > | 30000.0 | nM | - |