Assay Detail
Functional
CHEMBL986416
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A2A receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 8.51 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL472111 | — | — | 1 | 9.15 |
| CHEMBL472112 | — | — | 1 | 8.96 |
| CHEMBL512133 | — | — | 1 | 8.82 |
| CHEMBL470088 | — | — | 1 | 8.80 |
| CHEMBL470087 | — | — | 1 | 8.72 |
| CHEMBL469893 | — | — | 1 | 8.72 |
| CHEMBL472114 | — | — | 1 | 8.72 |
| CHEMBL17127 | SCH-58261 | — | 1 | 8.70 |
| CHEMBL472110 | — | — | 1 | 8.70 |
| CHEMBL471553 | — | — | 1 | 8.70 |
| CHEMBL513364 | — | — | 1 | 8.70 |
| CHEMBL510959 | — | — | 1 | 8.64 |
| CHEMBL469673 | — | — | 1 | 8.60 |
| CHEMBL470089 | — | — | 1 | 8.51 |
| CHEMBL469674 | — | — | 1 | 8.49 |
| CHEMBL512892 | — | — | 1 | 8.48 |
| CHEMBL469877 | — | — | 1 | 8.39 |
| CHEMBL471554 | — | — | 1 | 8.32 |
| CHEMBL511446 | — | — | 1 | 8.30 |
| CHEMBL512891 | — | — | 1 | 8.29 |
| CHEMBL469876 | — | — | 1 | 8.27 |
| CHEMBL471924 | — | — | 1 | 8.22 |
| CHEMBL513030 | — | — | 1 | 8.21 |
| CHEMBL469874 | — | — | 1 | 8.15 |
| CHEMBL471923 | — | — | 1 | 7.83 |
| CHEMBL469879 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL472111 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL472112 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL512133 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL470088 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL470087 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL469893 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL472114 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL17127 | SCH-58261 | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL472110 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL471553 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL513364 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL510959 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL469673 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL470089 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL469674 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL512892 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL469877 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL471554 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL511446 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL512891 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL469876 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL471924 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL513030 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL469874 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL471923 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL469879 | — | Ki | = | 17.9 | nM | 7.75 |