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JAK2 Gene Record

  • Summary
  • Interactions
  • Claims
  • JAK2 3717 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    3717
    JANUS KINASE 2
    JAK2
    JTK10
    THCYT3
    147796
    6192
    ENSG00000096968
    OTTHUMG00000019490
    O60674
    Tyrosine-protein kinase JAK2
    JAK-2
    JAK2_HUMAN
    TYROSINE-PROTEIN KINASE JAK2 (EC 2.7.1.112) (JANUS KINASE 2) (JAK-2). [SOURCE:UNIPROT/SWISSPROT;ACC:O60674]
    BE0002408
    JAK2 V617F
    JAK1/2
    28
    2048
    NM_004972
    NP_004963
    T08391

    Gene Info:

    Target Class Enzymes
    Target Subclass EC:2.7.10.2
    Initial Gene Query JAK
    Counted Citations from 1950-2000 3125
    Interpro Acc IPR001245
    Human Readable Name KINASE
    Human Readable Name DRUGGABLE GENOME
    Uniprot Status Swiss-Prot
    Uniprot Evidence 1: Evidence at protein level
    Interpro Type Domain
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    GuideToPharmacology Gene Category Name Janus kinase (JakA) family
    GuideToPharmacology Gene Category ID 581
    Gene Biotype PROTEIN_CODING
    (24 More Sources)

    Gene Categories: Category Details

    KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE
    ENZYME

    Publications:

    Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.
    Ding YY et al., 2018, Clinical efficacy of ruxolitinib and chemotherapy in a child with Philadelphia chromosome-like acute lymphoblastic leukemia with <i>GOLGA5-JAK2</i> fusion and induction failure., Haematologica
    Bercovich et al., 2008, Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome., Lancet
    Campbell et al., 2006, V617F mutation in JAK2 is associated with poorer survival in idiopathic myelofibrosis., Blood
    Marty et al., 2014, Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitors., Blood
    Wang et al., 2010, AML1 is overexpressed in patients with myeloproliferative neoplasms and mediates JAK2V617F-independent overexpression of NF-E2., Blood
    Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia
    Novotny-Diermayr et al., 2012, The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML., Blood Cancer J
    Baxter et al., Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders., Lancet
    Levine et al., 2005, The JAK2V617F activating mutation occurs in chronic myelomonocytic leukemia and acute myeloid leukemia, but not in acute lymphoblastic leukemia or chronic lymphocytic leukemia., Blood
    Weigert et al., 2012, Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition., J. Exp. Med.
    Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
    Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., Blood
    Passamonti et al., 2010, A prospective study of 338 patients with polycythemia vera: the impact of JAK2 (V617F) allele burden and leukocytosis on fibrotic or leukemic disease transformation and vascular complications., Leukemia
    Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
    Kilpivaara et al., 2009, A germline JAK2 SNP is associated with predisposition to the development of JAK2(V617F)-positive myeloproliferative neoplasms., Nat. Genet.
    Dusa et al., 2010, JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors., PLoS ONE
    Jekarl et al., 2010, JAK2 V617F mutation in myelodysplastic syndrome, myelodysplastic syndrome/myeloproliferative neoplasm, unclassifiable, refractory anemia with ring sideroblasts with thrombocytosis, and acute myeloid leukemia., Korean J Hematol
    Yoshiki et al., 2011, A case of myeloid sarcoma with correlation to JAK2V617F mutation, complicated by myelofibrosis and secondary acute myeloid leukemia., Intern. Med.
    Kiladjian et al., 2006, High molecular response rate of polycythemia vera patients treated with pegylated interferon alpha-2a., Blood
    Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
    Yang et al., 2012, Ruxolitinib: in the treatment of myelofibrosis., Drugs
    Chase et al., 2013, Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements., Haematologica
    Mullighan et al., 2009, JAK mutations in high-risk childhood acute lymphoblastic leukemia., Proc. Natl. Acad. Sci. U.S.A.
    Wernig et al., 2008, Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera., Cancer Cell
    Roug et al., 2011, A patient with a 20-year lag phase between JAK2-V617F+ myeloproliferation and NPM1-mutated AML arguing against a common origin of disease., Eur. J. Haematol.
    Paschka et al., 2013, Secondary genetic lesions in acute myeloid leukemia with inv(16) or t(16;16): a study of the German-Austrian AML Study Group (AMLSG)., Blood
    Hornakova et al., 2011, Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors., Haematologica
    Cervantes et al., 2013, Myelofibrosis: an update on current pharmacotherapy and future directions., Expert Opin Pharmacother
    Man et al., 2012, Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation., Blood
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Malak et al., Long term follow up of 93 families with myeloproliferative neoplasms: life expectancy and implications of JAK2V617F in the occurrence of complications., Blood Cells Mol. Dis.
    Rumi et al., 2014, Clinical effect of driver mutations of JAK2, CALR, or MPL in primary myelofibrosis., Blood
    Nagao et al., 2014, Proliferation and survival signaling from both Jak2-V617F and Lyn involving GSK3 and mTOR/p70S6K/4EBP1 in PVTL-1 cell line newly established from acute myeloid leukemia transformed from polycythemia vera., PLoS ONE
    Eghtedar et al., 2012, Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia., Blood
    Mazzacurati et al., 2015, The PIM inhibitor AZD1208 synergizes with ruxolitinib to induce apoptosis of ruxolitinib sensitive and resistant JAK2-V617F-driven cells and inhibit colony formation of primary MPN cells., Oncotarget
    Lierman et al., 2012, Ruxolitinib inhibits transforming JAK2 fusion proteins in vitro and induces complete cytogenetic remission in t(8;9)(p22;p24)/PCM1-JAK2-positive chronic eosinophilic leukemia., Blood
    Ismael et al., 2012, De novo childhood myelodysplastic/myeloproliferative disease with unique molecular characteristics., Br. J. Haematol.
    Pardanani A et al., 2011, Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis., J Clin Oncol
    Roskoski R Jr, 2016, Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases., Pharmacol Res
    Yang SH et al., 2011, Virtual screening and synthesis of quinazolines as novel JAK2 inhibitors., Bioorg Med Chem
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Kuriya B et al., 2017, Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential., Ther Adv Musculoskelet Dis
    Genovese MC et al., 2016, Baricitinib in Patients with Refractory Rheumatoid Arthritis., N Engl J Med
    Balko et al., 2016, Triple-negative breast cancers with amplification of JAK2 at the 9p24 locus demonstrate JAK2-specific dependence., Sci Transl Med
    Elling et al., 2011, Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease., Blood
    Hudkins RL et al., 2012, Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent., J Med Chem
    Tam CS et al., 2019, Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL., Blood
    Guo Y et al., 2019, Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase., J Med Chem
    Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
  • AC-430   JAK2

    Interaction Score: 2.91

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Novel Target
    Trial Name AC430
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

  • RUXOLITINIB   JAK2

    Interaction Score: 2.91

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type hematologic cancer
    Response Type decreased response
    Approval Status Preclinical

    PMIDs:
    29773603 18805579 16293597 24398328 20339092 21926964 22829971 15781101 16081687 22271575 26258521 22955920 20631743 25207766 19287384 20585391 21120162 22041374 16709929 24251790 23061804 22875628 19470474 18394554 21689158 23115274 21393331 23514013 22368270 25157968 22818858 24986690 24404189 22422826 26472029 22899477 22571758


    Sources:
    MyCancerGenomeClinicalTrial DTC OncoKB DoCM JAX-CKB CIViC TTD DrugBank MyCancerGenome GuideToPharmacology CGI

  • CHEMBL480411   JAK2

    Interaction Score: 1.46

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL500779   JAK2

    Interaction Score: 1.46

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • GANDOTINIB   JAK2

    Interaction Score: 1.46

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD MyCancerGenome GuideToPharmacology ChemblInteractions

  • XL-019   JAK2

    Interaction Score: 1.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

  • FEDRATINIB   JAK2

    Interaction Score: 1.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    21220608 18394554 27473820


    Sources:
    TdgClinicalTrial CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • MOMELOTINIB   JAK2

    Interaction Score: 1.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type resistant
    Evidence Type Actionable
    Approval Status Preclinical

    PMIDs:
    24398328 21926964


    Sources:
    JAX-CKB TTD GuideToPharmacology ChemblInteractions

  • LS-104   JAK2

    Interaction Score: 0.73

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AZD-1480   JAK2

    Interaction Score: 0.73

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type resistant

    PMIDs:
    21926964


    Sources:
    JAX-CKB TTD MyCancerGenome GuideToPharmacology ChemblInteractions

  • PACRITINIB   JAK2

    Interaction Score: 0.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name SB1518, ONX 0803
    Novel drug target Novel Target
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

  • BARICITINIB   JAK2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    28255337 27028914


    Sources:
    TTD DrugBank GuideToPharmacology ChemblInteractions

  • BMS-911543   JAK2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • NS-018   JAK2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • ITACITINIB   JAK2

    Interaction Score: 0.49

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • TOFACITINIB   JAK2

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    26258521 10592235


    Sources:
    DTC DrugBank GuideToPharmacology

  • CHEMBL2062804   JAK2

    Interaction Score: 0.36

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • RUXOLITINIB PHOSPHATE   JAK2

    Interaction Score: 0.36

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CT-1578   JAK2

    Interaction Score: 0.36

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • CHEMBL473773   JAK2

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL21156   JAK2

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • PEFICITINIB   JAK2

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • LESTAURTINIB   JAK2

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name lestaurtinib, CEP-701
    Novel drug target Novel Target
    Indication/Tumor Type hematologic cancer

    PMIDs:
    21926964


    Sources:
    JAX-CKB TdgClinicalTrial ChemblInteractions

  • CHEMBL71191   JAK2

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DECERNOTINIB   JAK2

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ABROCITINIB   JAK2

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • AT-9283   JAK2

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • SGI-1776   JAK2

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Indication/Tumor Type bone marrow cancer
    Response Type decreased response

    PMIDs:
    26472029


    Sources:
    JAX-CKB

  • SOLCITINIB   JAK2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • BREPOCITINIB   JAK2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • OCLACITINIB   JAK2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • FILGOTINIB   JAK2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TOFACITINIB CITRATE   JAK2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Janus Kinase (JAK) inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • DELGOCITINIB   JAK2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CERDULATINIB   JAK2

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • ZANUBRUTINIB   JAK2

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    31340982 31381333


    Sources:
    DrugBank

  • 6-AZAURIDINE   JAK2

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ZOTIRACICLIB   JAK2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • PEMBROLIZUMAB   JAK2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type predicted – resistant
    Approval Status Clinical Study

    PMIDs:
    27433843


    Sources:
    JAX-CKB CIViC COSMIC

  • REPOTRECTINIB   JAK2

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • UPADACITINIB   JAK2

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL1170485   JAK2

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL56543   JAK2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21185195


    Sources:
    DTC

  • CHEMBL29197   JAK2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CEP-11981   JAK2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22148921


    Sources:
    DTC

  • GIVINOSTAT   JAK2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • RGB-286638   JAK2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PICTILISIB   JAK2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy GDC-0941 + Ruxolitinib
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • TRIAMTERENE   JAK2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL53898   JAK2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TYRPHOSTIN 23   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DACTOLISIB   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BEZ235 + Ruxolitinib
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive

    PMIDs:
    24251790


    Sources:
    JAX-CKB

  • THIRAM   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ENMD-2076   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name ENMD-2076
    Novel drug target Novel Target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • JNJ-7706621   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Binding to the JH2 pseudo kinase domain of JAK2 was determined using isothermal titration calorimetry (ITC).
    Specific Action of the Ligand Binding
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • LAUROGUADINE   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SIROLIMUS   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22955920


    Sources:
    CIViC

  • ADAVOSERTIB   JAK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ENTRECTINIB   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC DrugBank

  • CHEMBL546797   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • IMATINIB   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type myeloid leukemia
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    21224473


    Sources:
    JAX-CKB

  • AST-487   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • GW843682X   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL1997335   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RG-1530   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • CHEMBL379975   JAK2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PACLITAXEL   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy NVP-BSK805 + paclitaxel
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type sensitive

    PMIDs:
    27075627


    Sources:
    JAX-CKB

  • PD-0166285   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ERLOTINIB   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TOZASERTIB   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DOVITINIB   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CYC-116   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAE-684   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PF-00562271   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   JAK2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • FOSTAMATINIB   JAK2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26516587


    Sources:
    DrugBank

  • Ensembl: ENSG00000096968

    • Version: 101_38

    Alternate Names:
    JAK2 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: O60674

    • Version: January-2014

    Alternate Names:
    JAK2 Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:2.7.10.2

    Publications:

  • RussLampel: ENSG00000096968

    • Version: 26-July-2011

    Alternate Names:
    TYROSINE-PROTEIN KINASE JAK2 (EC 2.7.1.112) (JANUS KINASE 2) (JAK-2). [SOURCE:UNIPROT/SWISSPROT;ACC:O60674] Description
    ENSG00000096968 Ensembl Gene Id
    JAK2 Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • BaderLabGenes: JAK2

    • Version: February-2014

    Alternate Names:
    3717 Entrez Gene ID

    Gene Info:
    Initial Gene Query JAK
    Counted Citations from 1950-2000 3125

    Gene Categories:
    KINASE

    Publications:

  • HopkinsGroom: O60674

    • Version: 11-September-2012

    Alternate Names:
    3717 Entrez Gene Id
    JAK2 Uniprot Gene Name
    ENSG00000096968 Ensembl Gene Id

    Gene Info:
    Interpro Acc IPR001245
    Human Readable Name KINASE
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • GuideToPharmacology: 3717

    • Version: 29-September-2020

    Alternate Names:
    6192 HUGO Gene ID
    6192 HUGO Gene Symbol
    Janus kinase 2 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Janus kinase (JakA) family
    GuideToPharmacology Gene Category ID 581

    Gene Categories:
    ENZYME

    Publications:

  • JAX-CKB: JAK2

    • Version: 27-September-2017

    Alternate Names:
    3717 CKB Entrez Id
    JAK2 CKB Gene Synonym
    JTK10 CKB Gene Synonym

    Gene Info:

    Publications:
    Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.
    Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia
    Marty et al., 2014, Germ-line JAK2 mutations in the kinase domain are responsible for hereditary thrombocytosis and are resistant to JAK2 and HSP90 inhibitors., Blood

  • CIViC: JAK2

    • Version: 14-September-2020

    Alternate Names:
    3717 Entrez Gene ID
    28 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:
    Wernig et al., 2008, Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera., Cancer Cell
    Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.
    Ding YY et al., 2018, Clinical efficacy of ruxolitinib and chemotherapy in a child with Philadelphia chromosome-like acute lymphoblastic leukemia with <i>GOLGA5-JAK2</i> fusion and induction failure., Haematologica

  • DrugBank: BE0002408

    • Version: 5.1.7

    Alternate Names:
    JAK2 DrugBank Gene Name
    O60674 UniProt Accession
    3717 Entrez Gene Id

    Gene Info:

    Publications:
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    Yang et al., 2012, Ruxolitinib: in the treatment of myelofibrosis., Drugs
    Cervantes et al., 2013, Myelofibrosis: an update on current pharmacotherapy and future directions., Expert Opin Pharmacother

  • CGI: JAK2

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Chase et al., 2013, Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements., Haematologica
    Lierman et al., 2012, Ruxolitinib inhibits transforming JAK2 fusion proteins in vitro and induces complete cytogenetic remission in t(8;9)(p22;p24)/PCM1-JAK2-positive chronic eosinophilic leukemia., Blood

  • DoCM: JAK2

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Bercovich et al., 2008, Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome., Lancet
    Campbell et al., 2006, V617F mutation in JAK2 is associated with poorer survival in idiopathic myelofibrosis., Blood
    Wang et al., 2010, AML1 is overexpressed in patients with myeloproliferative neoplasms and mediates JAK2V617F-independent overexpression of NF-E2., Blood

  • DTC: JAK2

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
    Hudkins RL et al., 2012, Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent., J Med Chem
    Yang SH et al., 2011, Virtual screening and synthesis of quinazolines as novel JAK2 inhibitors., Bioorg Med Chem

  • HingoraniCasas: ENSG00000096968

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000096968 Gene Symbol
    JAK2 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TALC: JAK2

    • Version: 12-May-2016

    Alternate Names:
    JAK2 Gene Symbol

    Gene Info:

    Publications:

  • MyCancerGenome: JAK2

    • Version: 20-Jun-2017

    Alternate Names:
    3717 Entrez Gene Id
    JAK2 MyCancerGenome Gene Symbol
    JAK2 MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • ChemblInteractions: JAK2

    • Version: chembl_23

    Alternate Names:
    JAK-2 UNIPROT
    JAK2 GENE_SYMBOL
    Tyrosine-protein kinase JAK2 UNIPROT

    Gene Info:

    Publications:

  • OncoKB: JAK2

    • Version: 23-July-2020

    Alternate Names:
    3717 OncoKB Entrez Id
    THCYT3 OncoKB Gene Synonym
    JTK10 OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Pharos: JAK2

    • Version: 03-September-2020

    Alternate Names:
    Tyrosine-protein kinase JAK2 Gene Name
    O60674 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • Tempus: JAK2

    • Version: 11-November-2018

    Alternate Names:
    JAK2 Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: JAK2

    • Version: 27-Jun-2013

    Alternate Names:
    3717 Gene ID
    JTK10 dGene Synonym
    THCYT3 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, TYROSINE KINASE

    Publications:

  • TTD: Janus kinase 2

    • Version: 2020.06.01

    Alternate Names:
    JAK-2 TTD Gene Abbreviation
    T08391 TTD Target ID

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: JAK2

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: JAK2

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FoundationOneGenes: JAK2

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: JAK2

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • GO: JAK2

    • Version: 05-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    TYROSINE KINASE

    Publications:

  • Oncomine: JAK2

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: JAK2

    • Version: 4-Sep-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21