Assay Detail
Binding
CHEMBL3868063
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Inhibition of GST-tagged recombinant human JAK2 expressed in baculovirus using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition after 30 mins by HTRF 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
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.44 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3940537 | — | — | 1 | 9.15 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.55 |
| CHEMBL3907087 | — | — | 1 | 8.05 |
| CHEMBL3970092 | — | — | 1 | 8.03 |
| CHEMBL3966342 | — | — | 1 | 7.98 |
| CHEMBL3948663 | — | — | 1 | 7.88 |
| CHEMBL3912973 | — | — | 1 | 7.78 |
| CHEMBL3895231 | — | — | 1 | 7.72 |
| CHEMBL3903955 | — | — | 1 | 7.59 |
| CHEMBL3950301 | — | — | 1 | 7.42 |
| CHEMBL3920857 | — | — | 1 | 7.37 |
| CHEMBL3922588 | — | — | 1 | 7.27 |
| CHEMBL3913592 | — | — | 1 | 7.26 |
| CHEMBL3895028 | — | — | 1 | 6.86 |
| CHEMBL3941571 | — | — | 1 | 6.79 |
| CHEMBL3974845 | — | — | 1 | 6.65 |
| CHEMBL3934182 | — | — | 1 | 6.49 |
| CHEMBL3955194 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3940537 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3907087 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3970092 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3966342 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3948663 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3912973 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL3895231 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL3903955 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL3950301 | — | IC50 | = | 37.9 | nM | 7.42 |
| CHEMBL3920857 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL3922588 | — | IC50 | = | 53.7 | nM | 7.27 |
| CHEMBL3913592 | — | IC50 | = | 55.4 | nM | 7.26 |
| CHEMBL3895028 | — | IC50 | = | 136.7 | nM | 6.86 |
| CHEMBL3941571 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3974845 | — | IC50 | = | 226.1 | nM | 6.65 |
| CHEMBL3934182 | — | IC50 | = | 324.5 | nM | 6.49 |
| CHEMBL3955194 | — | IC50 | = | 7089.0 | nM | 5.15 |