Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T08391 | ||||
Target Name | Janus kinase 2 (JAK-2) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | ITF2357 | Drug Info | IC50 = 1~10 nM | [3] | |
Ruxolitinib | Drug Info | IC50 = 4.5 nM | |||
Atropisomer 1 | Drug Info | IC50 = 270 nM | [1] | ||
NSC-1771 | Drug Info | IC50 = 223 nM | [2] | ||
Action against Disease Model | ITF2357 | Drug Info | The clonogenic activity of JAK2V617F mutated cells was inhibited by low concentrations of ITF2357 (IC50 0.001-0.01 mu M) | [3] | |
References | |||||
REF 1 | Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. J Med Chem. 2009 Dec 24;52(24):7938-41. | ||||
REF 2 | In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. | ||||
REF 3 | The histone deacetylase inhibitor ITF2357 selectively targets cells bearing mutated JAK2(V617F). Leukemia. 2008 Apr;22(4):740-7. | ||||
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