Assay Detail
Binding
CHEMBL933587
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Displacement of [3H]CPX from human recombinant adenosine A1 receptor expressed in CHO cells
39
Total Activities
39
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
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 6.32 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430050 | — | — | 1 | 7.12 |
| CHEMBL259524 | — | — | 1 | 6.81 |
| CHEMBL412747 | — | — | 1 | 6.78 |
| CHEMBL405901 | — | — | 1 | 6.75 |
| CHEMBL259300 | — | — | 1 | 6.73 |
| CHEMBL261554 | — | — | 1 | 6.70 |
| CHEMBL411452 | — | — | 1 | 6.66 |
| CHEMBL408266 | — | — | 1 | 6.58 |
| CHEMBL259342 | — | — | 1 | 6.56 |
| CHEMBL265212 | — | — | 1 | 6.56 |
| CHEMBL260976 | — | — | 1 | 6.54 |
| CHEMBL427911 | — | — | 1 | 6.52 |
| CHEMBL408936 | — | — | 1 | 6.50 |
| CHEMBL260490 | — | — | 1 | 6.46 |
| CHEMBL261817 | — | — | 1 | 6.46 |
| CHEMBL409852 | — | — | 1 | 6.46 |
| CHEMBL259130 | — | — | 1 | 6.45 |
| CHEMBL406775 | — | — | 1 | 6.42 |
| CHEMBL261525 | — | — | 1 | 6.39 |
| CHEMBL260763 | — | — | 1 | 6.38 |
| CHEMBL258507 | — | — | 1 | 6.37 |
| CHEMBL260975 | — | — | 1 | 6.36 |
| CHEMBL261526 | — | — | 1 | 6.28 |
| CHEMBL258686 | — | — | 1 | 6.24 |
| CHEMBL259129 | — | — | 1 | 6.21 |
| CHEMBL258499 | — | — | 1 | 6.20 |
| CHEMBL428086 | — | — | 1 | 6.04 |
| CHEMBL410529 | — | — | 1 | 5.95 |
| CHEMBL265213 | — | — | 1 | 5.92 |
| CHEMBL427736 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430050 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL259524 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL412747 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL405901 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL259300 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL261554 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL411452 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL408266 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL259342 | — | Ki | = | 274.0 | nM | 6.56 |
| CHEMBL265212 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL260976 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL427911 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL408936 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL409852 | — | Ki | = | 347.0 | nM | 6.46 |
| CHEMBL261817 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL260490 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL259130 | — | Ki | = | 352.0 | nM | 6.45 |
| CHEMBL406775 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL261525 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL260763 | — | Ki | = | 416.0 | nM | 6.38 |
| CHEMBL258507 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL260975 | — | Ki | = | 441.0 | nM | 6.36 |
| CHEMBL261526 | — | Ki | = | 522.0 | nM | 6.28 |
| CHEMBL258686 | — | Ki | = | 582.0 | nM | 6.24 |
| CHEMBL259129 | — | Ki | = | 617.0 | nM | 6.21 |
| CHEMBL258499 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL428086 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL410529 | — | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL265213 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL427736 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL261819 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL260878 | — | Ki | = | 1520.0 | nM | 5.82 |
| CHEMBL260933 | GS 6201 | Ki | = | 1940.0 | nM | 5.71 |
| CHEMBL407969 | — | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL259772 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL259565 | — | Ki | = | 3590.0 | nM | 5.45 |
| CHEMBL264952 | — | Ki | - | — | - | |
| CHEMBL410021 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL261182 | — | Ki | > | 6000.0 | nM | - |