Assay Detail
Binding
CHEMBL1292866
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Inhibition of human recombinant JAK2 by TR-FRET assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.54 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 8.52 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.52 |
| CHEMBL1287941 | — | — | 1 | 5.68 |
| CHEMBL1287883 | — | — | 1 | 5.60 |
| CHEMBL1288002 | — | — | 1 | 5.60 |
| CHEMBL1288001 | — | — | 1 | 5.30 |
| CHEMBL1287812 | — | — | 1 | - |
| CHEMBL1287910 | — | — | 1 | - |
| CHEMBL1287940 | — | — | 1 | - |
| CHEMBL1287970 | — | — | 1 | - |
| CHEMBL1288769 | — | — | 1 | - |
| CHEMBL1287971 | — | — | 1 | - |
| CHEMBL1288032 | — | — | 1 | - |
| CHEMBL1288033 | — | — | 1 | - |
| CHEMBL1288062 | — | — | 1 | - |
| CHEMBL1288063 | — | — | 1 | - |
| CHEMBL1288093 | — | — | 1 | - |
| CHEMBL1288094 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1287941 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL1287883 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1288002 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1288001 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1287812 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1287910 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1287940 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1287970 | — | IC50 | - | — | - | |
| CHEMBL1288769 | — | IC50 | - | — | - | |
| CHEMBL1287971 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL1288032 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1288033 | — | IC50 | - | — | - | |
| CHEMBL1288062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1288063 | — | IC50 | - | — | - | |
| CHEMBL1288093 | — | IC50 | - | — | - | |
| CHEMBL1288094 | — | IC50 | - | — | - |