Assay Detail
Binding
CHEMBL862546
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Displacement of [3H]MRE3008-F20 from human adenosine A3 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 | 8.59 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118923 | — | — | 1 | 10.85 |
| CHEMBL332091 | — | — | 1 | 10.34 |
| CHEMBL383714 | — | — | 1 | 9.46 |
| CHEMBL203797 | — | — | 1 | 9.36 |
| CHEMBL534936 | — | — | 1 | 9.30 |
| CHEMBL534489 | — | — | 1 | 9.26 |
| CHEMBL383689 | — | — | 1 | 8.89 |
| CHEMBL204753 | — | — | 1 | 8.46 |
| CHEMBL203998 | — | — | 1 | 8.46 |
| CHEMBL203660 | — | — | 1 | 8.28 |
| CHEMBL203060 | — | — | 1 | 8.00 |
| CHEMBL203506 | — | — | 1 | 8.00 |
| CHEMBL381123 | — | — | 1 | 7.96 |
| CHEMBL203054 | — | — | 1 | 7.92 |
| CHEMBL382665 | — | — | 1 | 7.80 |
| CHEMBL382357 | — | — | 1 | 7.68 |
| CHEMBL204128 | — | — | 1 | 7.55 |
| CHEMBL262987 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118923 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL332091 | — | Ki | = | 0.046 | nM | 10.34 |
| CHEMBL383714 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL203797 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL534936 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL534489 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL383689 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL204753 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL203998 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL203660 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL203060 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL203506 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL381123 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL203054 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL382665 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL382357 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL204128 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL262987 | — | Ki | = | 110.0 | nM | 6.96 |