Assay Detail
Binding
CHEMBL862544
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Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in HEK293 cells
18
Total Activities
18
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 | Expert |
Publication
Synthesis and biological studies of a new series of 5-heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.78 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203660 | — | — | 1 | 7.38 |
| CHEMBL203054 | — | — | 1 | 7.22 |
| CHEMBL383689 | — | — | 1 | 7.19 |
| CHEMBL332091 | — | — | 1 | 7.19 |
| CHEMBL203060 | — | — | 1 | 7.12 |
| CHEMBL203998 | — | — | 1 | 6.96 |
| CHEMBL118923 | — | — | 1 | 6.96 |
| CHEMBL203797 | — | — | 1 | 6.90 |
| CHEMBL383714 | — | — | 1 | 6.85 |
| CHEMBL382357 | — | — | 1 | 6.82 |
| CHEMBL534489 | — | — | 1 | 6.81 |
| CHEMBL534936 | — | — | 1 | 6.75 |
| CHEMBL204128 | — | — | 1 | 6.55 |
| CHEMBL382665 | — | — | 1 | 6.46 |
| CHEMBL381123 | — | — | 1 | 6.40 |
| CHEMBL204753 | — | — | 1 | 6.39 |
| CHEMBL262987 | — | — | 1 | 6.09 |
| CHEMBL203506 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203660 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL203054 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL383689 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL332091 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL203060 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL203998 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL118923 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL203797 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL383714 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL382357 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL534489 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL534936 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL204128 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL382665 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL381123 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL204753 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL262987 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL203506 | — | Ki | = | 920.0 | nM | 6.04 |