Assay Detail
Binding
CHEMBL864798
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Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatal membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.89 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL209366 | — | — | 1 | 7.64 |
| CHEMBL209230 | — | — | 1 | 7.57 |
| CHEMBL377246 | — | — | 1 | 7.38 |
| CHEMBL212625 | — | — | 1 | 7.03 |
| CHEMBL210585 | — | — | 1 | 6.95 |
| CHEMBL208550 | — | — | 1 | 6.78 |
| CHEMBL213878 | — | — | 1 | 6.74 |
| CHEMBL212626 | — | — | 1 | 6.55 |
| CHEMBL378102 | — | — | 1 | 6.54 |
| CHEMBL211521 | — | — | 1 | 6.53 |
| CHEMBL212217 | — | — | 1 | 6.50 |
| CHEMBL377106 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL209366 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL209230 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL377246 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL212625 | — | Ki | = | 93.7 | nM | 7.03 |
| CHEMBL210585 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL208550 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL213878 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL212626 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL378102 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL211521 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL212217 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL377106 | — | Ki | = | 347.0 | nM | 6.46 |