Assay Detail
Binding
CHEMBL5106115
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Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of subtype-selective covalent ligands for the adenosine A<sub>2B</sub> receptor by tuning the reactive group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.13 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5207498 | — | — | 1 | 8.67 |
| CHEMBL5207290 | — | — | 1 | 8.10 |
| CHEMBL5205220 | — | — | 1 | 7.93 |
| CHEMBL5196082 | — | — | 1 | 7.62 |
| CHEMBL5176227 | — | — | 1 | 7.31 |
| CHEMBL5172513 | — | — | 1 | 7.22 |
| CHEMBL5208506 | — | — | 1 | 6.96 |
| CHEMBL5195884 | — | — | 1 | 6.88 |
| CHEMBL5185103 | — | — | 1 | 6.85 |
| CHEMBL8565 | — | — | 1 | 6.71 |
| CHEMBL5172969 | — | — | 1 | 6.25 |
| CHEMBL5175698 | — | — | 1 | 6.21 |
| CHEMBL5198830 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5207498 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL5207290 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL5205220 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL5196082 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL5176227 | — | Ki | = | 48.98 | nM | 7.31 |
| CHEMBL5172513 | — | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL5208506 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL5195884 | — | Ki | = | 131.83 | nM | 6.88 |
| CHEMBL5185103 | — | Ki | = | 141.25 | nM | 6.85 |
| CHEMBL8565 | — | Ki | = | 194.98 | nM | 6.71 |
| CHEMBL5172969 | — | Ki | = | 562.34 | nM | 6.25 |
| CHEMBL5175698 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL5198830 | — | Ki | = | 954.99 | nM | 6.02 |