Assay Detail
Binding
CHEMBL829690
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Inhibition of [3H]MRE3008-F20 binding to human adenosine A3 receptor expressed in CHO cells; (n=3 - 6)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.26 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188035 | — | — | 1 | 8.05 |
| CHEMBL363150 | — | — | 1 | 7.80 |
| CHEMBL364786 | — | — | 1 | 7.72 |
| CHEMBL364319 | — | — | 1 | 7.57 |
| CHEMBL363516 | — | — | 1 | 7.57 |
| CHEMBL187766 | — | — | 1 | 7.36 |
| CHEMBL190612 | — | — | 1 | 6.90 |
| CHEMBL188436 | — | — | 1 | 6.80 |
| CHEMBL188052 | — | — | 1 | 6.78 |
| CHEMBL190111 | — | — | 1 | 6.67 |
| CHEMBL187842 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188035 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL363150 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL364786 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL364319 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL363516 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL187766 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL190612 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL188436 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL188052 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL190111 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL187842 | — | Ki | = | 220.0 | nM | 6.66 |