Assay Detail
Binding
CHEMBL870047
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Displacement of [125I]I-AB-MECA from human adenosine A3 receptor H272E mutant expressed in COS7 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.38 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382812 | — | — | 1 | 6.73 |
| CHEMBL377071 | — | — | 1 | 6.73 |
| CHEMBL377490 | — | — | 1 | 6.70 |
| CHEMBL382194 | — | — | 1 | 6.66 |
| CHEMBL2113221 | — | — | 1 | 6.64 |
| CHEMBL208475 | — | — | 1 | 6.23 |
| CHEMBL144521 | — | — | 1 | 6.21 |
| CHEMBL207610 | — | — | 1 | 6.16 |
| CHEMBL378069 | — | — | 1 | 6.15 |
| CHEMBL206085 | — | — | 1 | 5.57 |
| CHEMBL378606 | — | — | 1 | - |
| CHEMBL129903 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382812 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL377071 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL377490 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL382194 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL2113221 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL208475 | — | Ki | = | 592.0 | nM | 6.23 |
| CHEMBL144521 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL207610 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL378069 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL206085 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL378606 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL129903 | — | Ki | > | 100000.0 | nM | - |