Assay Detail
Binding
CHEMBL840030
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Inhibition of [3H]DPCPX binding to adenosine A1 receptor of rat cerebral cortex
39
Total Activities
39
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
Novel diamino 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 | 39 | 6.15 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17127 | SCH-58261 | — | 1 | 6.41 |
| CHEMBL113142 | ZM-241385 | — | 1 | 6.17 |
| CHEMBL27508 | — | — | 1 | 6.03 |
| CHEMBL177943 | — | — | 1 | 6.00 |
| CHEMBL177229 | — | — | 1 | - |
| CHEMBL177609 | — | — | 1 | - |
| CHEMBL177711 | — | — | 1 | - |
| CHEMBL368488 | — | — | 1 | - |
| CHEMBL368619 | — | — | 1 | - |
| CHEMBL368620 | — | — | 1 | - |
| CHEMBL177459 | — | — | 1 | - |
| CHEMBL359641 | — | — | 1 | - |
| CHEMBL175645 | — | — | 1 | - |
| CHEMBL175298 | — | — | 1 | - |
| CHEMBL368827 | — | — | 1 | - |
| CHEMBL368070 | — | — | 1 | - |
| CHEMBL175818 | — | — | 1 | - |
| CHEMBL177539 | — | — | 1 | - |
| CHEMBL174628 | — | — | 1 | - |
| CHEMBL177386 | — | — | 1 | - |
| CHEMBL179478 | — | — | 1 | - |
| CHEMBL369550 | — | — | 1 | - |
| CHEMBL369373 | — | — | 1 | - |
| CHEMBL361229 | — | — | 1 | - |
| CHEMBL426782 | — | — | 1 | - |
| CHEMBL369070 | — | — | 1 | - |
| CHEMBL175564 | — | — | 1 | - |
| CHEMBL367593 | — | — | 1 | - |
| CHEMBL173941 | — | — | 1 | - |
| CHEMBL177615 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17127 | SCH-58261 | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL113142 | ZM-241385 | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL27508 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL177943 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL177459 | — | Ki | > | 250.0 | nM | - |
| CHEMBL176071 | — | Ki | > | 250.0 | nM | - |
| CHEMBL359641 | — | Ki | > | 250.0 | nM | - |
| CHEMBL175645 | — | Ki | > | 250.0 | nM | - |
| CHEMBL175298 | — | Ki | > | 250.0 | nM | - |
| CHEMBL368827 | — | Ki | > | 250.0 | nM | - |
| CHEMBL368070 | — | Ki | > | 1700.0 | nM | - |
| CHEMBL175818 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177609 | — | Ki | > | 250.0 | nM | - |
| CHEMBL368201 | — | Ki | > | 250.0 | nM | - |
| CHEMBL368382 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177532 | — | Ki | > | 250.0 | nM | - |
| CHEMBL173993 | — | Ki | > | 250.0 | nM | - |
| CHEMBL173672 | — | Ki | > | 430.0 | nM | - |
| CHEMBL177859 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177446 | — | Ki | > | 250.0 | nM | - |
| CHEMBL176039 | — | Ki | > | 800.0 | nM | - |
| CHEMBL369550 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177615 | — | Ki | > | 250.0 | nM | - |
| CHEMBL173941 | — | Ki | > | 1300.0 | nM | - |
| CHEMBL367593 | — | Ki | > | 250.0 | nM | - |
| CHEMBL175564 | — | Ki | > | 250.0 | nM | - |
| CHEMBL369070 | — | Ki | > | 250.0 | nM | - |
| CHEMBL426782 | — | Ki | > | 250.0 | nM | - |
| CHEMBL361229 | — | Ki | > | 250.0 | nM | - |
| CHEMBL369373 | — | Ki | > | 250.0 | nM | - |
| CHEMBL368620 | — | Ki | > | 250.0 | nM | - |
| CHEMBL179478 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177386 | — | Ki | > | 250.0 | nM | - |
| CHEMBL174628 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177539 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177229 | — | Ki | > | 250.0 | nM | - |
| CHEMBL177711 | — | Ki | > | 500.0 | nM | - |
| CHEMBL368488 | — | Ki | > | 500.0 | nM | - |
| CHEMBL368619 | — | Ki | > | 2900.0 | nM | - |