Assay Detail
Binding
CHEMBL840033
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Inhibition of [3H]DPCPX binding to rat cerebral cortex adenosine A1 receptor
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 6.01 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL185967 | — | — | 1 | 6.60 |
| CHEMBL186027 | — | — | 1 | 6.44 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.41 |
| CHEMBL189453 | — | — | 1 | 6.38 |
| CHEMBL186022 | — | — | 1 | 6.30 |
| CHEMBL188898 | — | — | 1 | 6.19 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.17 |
| CHEMBL361275 | — | — | 1 | 6.17 |
| CHEMBL187586 | — | — | 1 | 6.17 |
| CHEMBL360178 | — | — | 1 | 6.14 |
| CHEMBL188424 | — | — | 1 | 6.08 |
| CHEMBL27508 | — | — | 1 | 6.03 |
| CHEMBL189192 | — | — | 1 | 5.96 |
| CHEMBL173941 | — | — | 1 | 5.89 |
| CHEMBL359772 | — | — | 1 | 5.89 |
| CHEMBL187366 | — | — | 1 | 5.82 |
| CHEMBL361680 | — | — | 1 | 5.57 |
| CHEMBL368619 | — | — | 1 | 5.54 |
| CHEMBL186046 | — | — | 1 | 5.35 |
| CHEMBL186023 | — | — | 1 | 5.13 |
| CHEMBL188982 | — | — | 1 | - |
| CHEMBL186725 | — | — | 1 | - |
| CHEMBL188305 | — | — | 1 | - |
| CHEMBL364612 | — | — | 1 | - |
| CHEMBL177711 | — | — | 1 | - |
| CHEMBL368488 | — | — | 1 | - |
| CHEMBL186322 | — | — | 1 | - |
| CHEMBL426068 | — | — | 1 | - |
| CHEMBL186885 | — | — | 1 | - |
| CHEMBL188897 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL185967 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL186027 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL17127 | SCH-58261 | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL189453 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL186022 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL188898 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL113142 | ZM-241385 | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL361275 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL187586 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL360178 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL188424 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL27508 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL189192 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL173941 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL359772 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL187366 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL361680 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL368619 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL186046 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL186023 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL188564 | — | Ki | > | 500.0 | nM | - |
| CHEMBL188470 | — | Ki | - | nM | - | |
| CHEMBL364988 | — | Ki | - | nM | - | |
| CHEMBL186293 | — | Ki | > | 500.0 | nM | - |
| CHEMBL362513 | — | Ki | > | 500.0 | nM | - |
| CHEMBL175927 | — | Ki | > | 500.0 | nM | - |
| CHEMBL445139 | — | Ki | > | 500.0 | nM | - |
| CHEMBL186003 | — | Ki | > | 500.0 | nM | - |
| CHEMBL189293 | — | Ki | > | 500.0 | nM | - |
| CHEMBL186234 | — | Ki | > | 500.0 | nM | - |
| CHEMBL365303 | — | Ki | > | 500.0 | nM | - |
| CHEMBL425349 | — | Ki | - | nM | - | |
| CHEMBL185888 | — | Ki | > | 500.0 | nM | - |
| CHEMBL188897 | — | Ki | > | 500.0 | nM | - |
| CHEMBL186885 | — | Ki | > | 500.0 | nM | - |
| CHEMBL426068 | — | Ki | > | 500.0 | nM | - |
| CHEMBL186322 | — | Ki | > | 500.0 | nM | - |
| CHEMBL368488 | — | Ki | > | 500.0 | nM | - |
| CHEMBL177711 | — | Ki | > | 500.0 | nM | - |
| CHEMBL364612 | — | Ki | > | 500.0 | nM | - |
| CHEMBL188305 | — | Ki | > | 500.0 | nM | - |
| CHEMBL186725 | — | Ki | > | 500.0 | nM | - |
| CHEMBL188982 | — | Ki | > | 500.0 | nM | - |