Assay Detail
Binding
CHEMBL991729
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Displacement of [3H]NECA from Sprague-Dawley rat adenosine A2A receptor by scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.30 | 8.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489592 | — | — | 1 | 8.56 |
| CHEMBL431770 | ISTRADEFYLLINE | 4.0 | 1 | 8.35 |
| CHEMBL490014 | — | — | 1 | 8.11 |
| CHEMBL446316 | — | — | 1 | 7.87 |
| CHEMBL483243 | — | — | 1 | 7.52 |
| CHEMBL522256 | — | — | 1 | 7.23 |
| CHEMBL489390 | — | — | 1 | 6.98 |
| CHEMBL489391 | — | — | 1 | 6.94 |
| CHEMBL483663 | — | — | 1 | 6.82 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489592 | — | Ki | = | 2.74 | nM | 8.56 |
| CHEMBL431770 | ISTRADEFYLLINE | Ki | = | 4.46 | nM | 8.35 |
| CHEMBL490014 | — | Ki | = | 7.73 | nM | 8.11 |
| CHEMBL446316 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL483243 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL522256 | — | Ki | = | 59.1 | nM | 7.23 |
| CHEMBL489390 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL489391 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL483663 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL113 | CAFFEINE | Ki | = | 22000.0 | nM | 4.66 |