Assay Detail
Binding
CHEMBL5706195
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Inhibition of GST tagged JAK2 (unknown origin) expressed in insect cells
5
Total Activities
5
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.46 | 9.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | EFO:0002429 |
| EFO_TERM | EFO_TERM | - | — | polycythemia vera |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 9.00 |
| CHEMBL4294155 | — | — | 1 | 8.70 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 8.52 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 8.35 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4294155 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1078178 | MOMELOTINIB | IC50 | = | 18.0 | nM | 7.75 |