Assay Detail
Binding
CHEMBL1024508
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Displacement of [3H]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting
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 | Intermediate |
Publication
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.52 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200732 | — | — | 1 | 9.42 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.85 |
| CHEMBL413686 | — | — | 1 | 8.38 |
| CHEMBL561976 | — | — | 1 | 7.89 |
| CHEMBL554275 | — | — | 1 | 7.43 |
| CHEMBL558891 | — | — | 1 | 7.37 |
| CHEMBL561855 | — | — | 1 | 7.23 |
| CHEMBL538639 | — | — | 1 | 7.15 |
| CHEMBL564676 | — | — | 1 | 7.12 |
| CHEMBL549563 | — | — | 1 | 7.12 |
| CHEMBL549352 | — | — | 1 | 7.04 |
| CHEMBL563359 | — | — | 1 | 6.55 |
| CHEMBL564883 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200732 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL413686 | — | Ki | = | 4.16 | nM | 8.38 |
| CHEMBL561976 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL554275 | — | Ki | = | 37.5 | nM | 7.43 |
| CHEMBL558891 | — | Ki | = | 42.9 | nM | 7.37 |
| CHEMBL561855 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL538639 | — | Ki | = | 70.1 | nM | 7.15 |
| CHEMBL564676 | — | Ki | = | 76.1 | nM | 7.12 |
| CHEMBL549563 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL549352 | — | Ki | = | 90.2 | nM | 7.04 |
| CHEMBL563359 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL564883 | — | Ki | = | 537.0 | nM | 6.27 |