Assay Detail
Binding
CHEMBL3123571
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Displacement of [3H]-HEMADO from human recombinant adenosine A3 receptor expressed in CHO cell membranes after 3 hrs by microbeta counting analysis
13
Total Activities
13
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 | Autocuration |
Publication
Novel 8-(p-substituted-phenyl/benzyl)xanthines with selectivity for the A2A adenosine receptor possess bronchospasmolytic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.30 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3121727 | — | — | 1 | 8.64 |
| CHEMBL3121723 | — | — | 1 | 8.56 |
| CHEMBL3121724 | — | — | 1 | 8.34 |
| CHEMBL3121722 | — | — | 1 | 8.19 |
| CHEMBL3121721 | — | — | 1 | 8.17 |
| CHEMBL3121728 | — | — | 1 | 8.16 |
| CHEMBL3121720 | — | — | 1 | 8.03 |
| CHEMBL3121732 | — | — | 1 | - |
| CHEMBL3121731 | — | — | 1 | - |
| CHEMBL3121730 | — | — | 1 | - |
| CHEMBL3121729 | — | — | 1 | - |
| CHEMBL3121725 | — | — | 1 | - |
| CHEMBL3121726 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3121727 | — | Ki | = | 2.27 | nM | 8.64 |
| CHEMBL3121723 | — | Ki | = | 2.74 | nM | 8.56 |
| CHEMBL3121724 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3121722 | — | Ki | = | 6.51 | nM | 8.19 |
| CHEMBL3121721 | — | Ki | = | 6.82 | nM | 8.17 |
| CHEMBL3121728 | — | Ki | = | 6.89 | nM | 8.16 |
| CHEMBL3121720 | — | Ki | = | 9.38 | nM | 8.03 |
| CHEMBL3121732 | — | Ki | > | 30.0 | nM | - |
| CHEMBL3121731 | — | Ki | > | 30.0 | nM | - |
| CHEMBL3121730 | — | Ki | > | 30.0 | nM | - |
| CHEMBL3121729 | — | Ki | > | 30.0 | nM | - |
| CHEMBL3121725 | — | Ki | > | 30.0 | nM | - |
| CHEMBL3121726 | — | Ki | > | 10.0 | nM | - |