Assay Detail
Binding
CHEMBL829684
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Inhibition of [3H]ZM-241,385 binding to rat brain adenosine A2a receptor
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 7.22 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | — | 1 | 9.05 |
| CHEMBL187586 | — | — | 1 | 8.70 |
| CHEMBL173941 | — | — | 1 | 8.52 |
| CHEMBL186022 | — | — | 1 | 8.30 |
| CHEMBL185967 | — | — | 1 | 8.22 |
| CHEMBL187366 | — | — | 1 | 8.00 |
| CHEMBL186027 | — | — | 1 | 7.92 |
| CHEMBL189192 | — | — | 1 | 7.85 |
| CHEMBL426068 | — | — | 1 | 7.80 |
| CHEMBL188424 | — | — | 1 | 7.75 |
| CHEMBL368619 | — | — | 1 | 7.75 |
| CHEMBL359772 | — | — | 1 | 7.52 |
| CHEMBL364988 | — | — | 1 | 7.46 |
| CHEMBL186234 | — | — | 1 | 7.44 |
| CHEMBL17127 | SCH-58261 | — | 1 | 7.43 |
| CHEMBL27508 | — | — | 1 | 7.38 |
| CHEMBL188564 | — | — | 1 | 7.33 |
| CHEMBL189293 | — | — | 1 | 7.32 |
| CHEMBL360178 | — | — | 1 | 7.27 |
| CHEMBL361275 | — | — | 1 | 7.24 |
| CHEMBL189453 | — | — | 1 | 7.24 |
| CHEMBL365303 | — | — | 1 | 7.14 |
| CHEMBL188898 | — | — | 1 | 7.13 |
| CHEMBL188470 | — | — | 1 | 7.12 |
| CHEMBL186023 | — | — | 1 | 7.07 |
| CHEMBL186885 | — | — | 1 | 7.02 |
| CHEMBL361680 | — | — | 1 | 6.96 |
| CHEMBL186046 | — | — | 1 | 6.94 |
| CHEMBL362513 | — | — | 1 | 6.89 |
| CHEMBL186003 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL187586 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL173941 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL186022 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL185967 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL187366 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL186027 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL189192 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL426068 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL188424 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL368619 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL359772 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL364988 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL186234 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL17127 | SCH-58261 | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL27508 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL188564 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL189293 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL360178 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL361275 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL189453 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL365303 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL188898 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL188470 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL186023 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL186885 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL361680 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL186046 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL362513 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL186003 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL188897 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL175927 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL177711 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL185888 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL186293 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL445139 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL364612 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL188982 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL186322 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL368488 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL188305 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL186725 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL425349 | — | Ki | > | 5000.0 | nM | - |