Assay Detail
Binding
CHEMBL864795
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Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical 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 | 7.59 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL209366 | — | — | 1 | 8.74 |
| CHEMBL209230 | — | — | 1 | 8.34 |
| CHEMBL377246 | — | — | 1 | 8.26 |
| CHEMBL211521 | — | — | 1 | 8.00 |
| CHEMBL210585 | — | — | 1 | 7.92 |
| CHEMBL208550 | — | — | 1 | 7.57 |
| CHEMBL378102 | — | — | 1 | 7.35 |
| CHEMBL213878 | — | — | 1 | 7.19 |
| CHEMBL212626 | — | — | 1 | 7.12 |
| CHEMBL377106 | — | — | 1 | 7.01 |
| CHEMBL212217 | — | — | 1 | 7.00 |
| CHEMBL212625 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL209366 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL209230 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL377246 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL211521 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL210585 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL208550 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL378102 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL213878 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL212626 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL377106 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL212217 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL212625 | — | Ki | = | 260.0 | nM | 6.58 |