Assay Detail
Binding
CHEMBL642184
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Displacement of [3H]MSX-2 from adenosine A2A receptor of rat brain striatal membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.87 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8865 | — | — | 1 | 7.80 |
| CHEMBL8810 | — | — | 1 | 7.68 |
| CHEMBL266099 | — | — | 1 | 7.55 |
| CHEMBL417601 | — | — | 1 | 7.47 |
| CHEMBL8495 | — | — | 1 | 7.27 |
| CHEMBL267474 | — | — | 1 | 7.20 |
| CHEMBL8732 | — | — | 1 | 7.13 |
| CHEMBL412854 | — | — | 1 | 7.11 |
| CHEMBL9030 | — | — | 1 | 7.00 |
| CHEMBL9034 | — | — | 1 | 6.93 |
| CHEMBL8789 | — | — | 1 | 6.19 |
| CHEMBL268617 | — | — | 1 | 5.09 |
| CHEMBL8565 | — | — | 1 | 4.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8865 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL8810 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL266099 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL417601 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL8495 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL267474 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL8732 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL412854 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL9030 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL9034 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL8789 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL268617 | — | Ki | = | 8070.0 | nM | 5.09 |
| CHEMBL8565 | — | Ki | = | 11800.0 | nM | 4.93 |