Assay Detail
Binding
CHEMBL933588
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Displacement of [3H]ZM-241385 from human recombinant adenosine A2A receptor expressed in HEK293 cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 6.26 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL259300 | — | — | 1 | 7.14 |
| CHEMBL408266 | — | — | 1 | 7.14 |
| CHEMBL258686 | — | — | 1 | 6.90 |
| CHEMBL260976 | — | — | 1 | 6.86 |
| CHEMBL259524 | — | — | 1 | 6.83 |
| CHEMBL408936 | — | — | 1 | 6.74 |
| CHEMBL427911 | — | — | 1 | 6.66 |
| CHEMBL260490 | — | — | 1 | 6.64 |
| CHEMBL259342 | — | — | 1 | 6.63 |
| CHEMBL430050 | — | — | 1 | 6.63 |
| CHEMBL260763 | — | — | 1 | 6.61 |
| CHEMBL265212 | — | — | 1 | 6.58 |
| CHEMBL411452 | — | — | 1 | 6.57 |
| CHEMBL259130 | — | — | 1 | 6.52 |
| CHEMBL412747 | — | — | 1 | 6.51 |
| CHEMBL261526 | — | — | 1 | 6.51 |
| CHEMBL409852 | — | — | 1 | 6.39 |
| CHEMBL261525 | — | — | 1 | 6.39 |
| CHEMBL260975 | — | — | 1 | 6.35 |
| CHEMBL258507 | — | — | 1 | 6.32 |
| CHEMBL405901 | — | — | 1 | 6.30 |
| CHEMBL259129 | — | — | 1 | 6.20 |
| CHEMBL260878 | — | — | 1 | 6.17 |
| CHEMBL261554 | — | — | 1 | 6.11 |
| CHEMBL258499 | — | — | 1 | 5.96 |
| CHEMBL261817 | — | — | 1 | 5.91 |
| CHEMBL406775 | — | — | 1 | 5.86 |
| CHEMBL410529 | — | — | 1 | 5.71 |
| CHEMBL259772 | — | — | 1 | 5.65 |
| CHEMBL427736 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL259300 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL408266 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL258686 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL260976 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL259524 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL408936 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL427911 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL260490 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL259342 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL430050 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL260763 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL265212 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL411452 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL259130 | — | Ki | = | 301.0 | nM | 6.52 |
| CHEMBL261526 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL412747 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL409852 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL261525 | — | Ki | = | 411.0 | nM | 6.39 |
| CHEMBL260975 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL258507 | — | Ki | = | 481.0 | nM | 6.32 |
| CHEMBL405901 | — | Ki | = | 496.0 | nM | 6.30 |
| CHEMBL259129 | — | Ki | = | 633.0 | nM | 6.20 |
| CHEMBL260878 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL261554 | — | Ki | = | 781.0 | nM | 6.11 |
| CHEMBL258499 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL261817 | — | Ki | = | 1220.0 | nM | 5.91 |
| CHEMBL406775 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL410529 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL259772 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL427736 | — | Ki | = | 2280.0 | nM | 5.64 |
| CHEMBL407969 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL265213 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL260933 | GS 6201 | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL428086 | — | Ki | = | 3780.0 | nM | 5.42 |
| CHEMBL261819 | — | Ki | = | 3850.0 | nM | 5.42 |
| CHEMBL259565 | — | Ki | = | 5410.0 | nM | 5.27 |
| CHEMBL410021 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL261182 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL264952 | — | Ki | - | — | - |