Assay Detail
Binding
CHEMBL1024667
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Displacement of [3H]SCH58261 from human adenosine A2A receptor expressed in HEK293 cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 8.66 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL480570 | — | — | 1 | 9.52 |
| CHEMBL480542 | — | — | 1 | 9.52 |
| CHEMBL470942 | — | — | 1 | 9.52 |
| CHEMBL514939 | — | — | 1 | 9.30 |
| CHEMBL480380 | — | — | 1 | 9.15 |
| CHEMBL473440 | — | — | 1 | 9.15 |
| CHEMBL512337 | — | — | 1 | 9.10 |
| CHEMBL473431 | — | — | 1 | 9.05 |
| CHEMBL363660 | — | — | 1 | 9.00 |
| CHEMBL519271 | — | — | 1 | 9.00 |
| CHEMBL521242 | — | — | 1 | 8.85 |
| CHEMBL473439 | — | — | 1 | 8.82 |
| CHEMBL361687 | — | — | 1 | 8.82 |
| CHEMBL480568 | — | — | 1 | 8.82 |
| CHEMBL475445 | — | — | 1 | 8.80 |
| CHEMBL482329 | — | — | 1 | 8.74 |
| CHEMBL481736 | — | — | 1 | 8.74 |
| CHEMBL520286 | — | — | 1 | 8.70 |
| CHEMBL480756 | — | — | 1 | 8.60 |
| CHEMBL480556 | — | — | 1 | 8.55 |
| CHEMBL481737 | — | — | 1 | 8.55 |
| CHEMBL482161 | — | — | 1 | 8.52 |
| CHEMBL520766 | — | — | 1 | 8.24 |
| CHEMBL471976 | — | — | 1 | 8.24 |
| CHEMBL480397 | — | — | 1 | 8.22 |
| CHEMBL480749 | — | — | 1 | 8.02 |
| CHEMBL471974 | — | — | 1 | 7.94 |
| CHEMBL482328 | — | — | 1 | 7.60 |
| CHEMBL475592 | — | — | 1 | 7.40 |
| CHEMBL471975 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL480570 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL480542 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL470942 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL514939 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL480380 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL473440 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL512337 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL473431 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL363660 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL519271 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL521242 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL473439 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL361687 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL480568 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL475445 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL482329 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL481736 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL520286 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL480756 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL480556 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL481737 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL482161 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL520766 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL471976 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL480397 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL480749 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL471974 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL482328 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL475592 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL471975 | — | Ki | = | 46.0 | nM | 7.34 |