DGIdb - JAK2 Gene Record

JAK2 3717 Druggable GenomeClinically Actionable

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
TTDC00187
NM_004972
NP_004963
T08391

Gene Info:

Source Reported Gene Name	JAK2
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
Human Readable Name	TYROSINE KINASE
GuideToPharmacology Gene Category Name	Janus kinase (JakA) family
GuideToPharmacology Gene Category ID	581
GuideToPharmacology Gene Type	enzyme
Gene Biotype	PROTEIN_CODING

(24 More Sources)

Gene Categories: Category Details

PROTEIN PHOSPHATASE
KINASE
SERINE THREONINE KINASE
TYROSINE KINASE
HISTONE MODIFICATION
PROTEASE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.
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
Hornakova et al., 2011, Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors., Haematologica
Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia
Weigert et al., 2012, Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition., J. Exp. Med.
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
Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
Dusa et al., 2010, JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors., PLoS ONE
Bercovich et al., 2008, Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome., Lancet
Maude et al., 2012, Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia., Blood
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
Mullighan et al., 2009, JAK mutations in high-risk childhood acute lymphoblastic leukemia., Proc. Natl. Acad. Sci. U.S.A.
Kilpivaara et al., 2009, A germline JAK2 SNP is associated with predisposition to the development of JAK2(V617F)-positive myeloproliferative neoplasms., Nat. Genet.
Kiladjian et al., 2006, High molecular response rate of polycythemia vera patients treated with pegylated interferon alpha-2a., Blood
Ismael et al., 2012, De novo childhood myelodysplastic/myeloproliferative disease with unique molecular characteristics., Br. 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
Wernig et al., 2008, Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera., Cancer Cell
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
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Rumi et al., 2014, Clinical effect of driver mutations of JAK2, CALR, or MPL in primary myelofibrosis., Blood
Yoshiki et al., 2011, A case of myeloid sarcoma with correlation to JAK2V617F mutation, complicated by myelofibrosis and secondary acute myeloid leukemia., Intern. Med.
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
Wang et al., 2010, AML1 is overexpressed in patients with myeloproliferative neoplasms and mediates JAK2V617F-independent overexpression of NF-E2., Blood
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
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.
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
Campbell et al., 2006, V617F mutation in JAK2 is associated with poorer survival in idiopathic myelofibrosis., Blood
Baxter et al., Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders., Lancet
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
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.
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
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
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
Chase et al., 2013, Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements., Haematologica
Kesarwani M et al., 2015, Targeting substrate-site in Jak2 kinase prevents emergence of genetic resistance., Sci Rep
Patel AB et al., 2019, JAK2 ex13InDel drives oncogenic transformation and is associated with chronic eosinophilic leukemia and polycythemia vera., Blood
Sadras T et al., 2017, A novel somatic JAK2 kinase-domain mutation in pediatric acute lymphoblastic leukemia with rapid on-treatment development of LOH., Cancer Genet
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
Nakaya et al., 2011, Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms., Blood Cancer J
Verstovsek S et al., 2017, A phase 1 study of the Janus kinase 2 (JAK2)<sup>V617F</sup> inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia., Leuk Res
Purandare AV et al., 2012, Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2., Leukemia
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.
Genovese MC et al., 2016, Baricitinib in Patients with Refractory Rheumatoid Arthritis., N Engl J Med
Kuriya B et al., 2017, Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential., Ther Adv Musculoskelet Dis
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

FEDRATINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

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

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

Kesarwani M et al., 2015, Targeting substrate-site in Jak2 kinase prevents emergence of genetic resistance., Sci Rep

NS-018 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Nakaya et al., 2011, Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms., Blood Cancer J
AZD-1480 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type resistant

Publications:

Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

GANDOTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Verstovsek S et al., 2017, A phase 1 study of the Janus kinase 2 (JAK2)<sup>V617F</sup> inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia., Leuk Res

BMS-911543 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Specific Action of the Ligand Inhibition

Publications:

Purandare AV et al., 2012, Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2., Leukemia
LESTAURTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name lestaurtinib, CEP-701

Novel drug target Novel Target

Indication/Tumor Type hematologic cancer

Publications:

Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

MOMELOTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Evidence Type Actionable

Approval Status Preclinical

Publications:

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

Patel AB et al., 2019, JAK2 ex13InDel drives oncogenic transformation and is associated with chronic eosinophilic leukemia and polycythemia vera., Blood

BARICITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Genovese MC et al., 2016, Baricitinib in Patients with Refractory Rheumatoid Arthritis., N Engl J Med

Kuriya B et al., 2017, Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential., Ther Adv Musculoskelet Dis

CERDULATINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
ZOTIRACICLIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:
ITACITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
RG-1530 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
CT-1578 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Publications:
AC-430 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name AC430

Direct Interaction? False

Publications:

JNJ-7706621 JAK2

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

Publications:

RUXOLITINIB PHOSPHATE JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Publications:
DELGOCITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
XL-019 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:
AT-9283 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
PACRITINIB JAK2

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

Publications:
TOFACITINIB CITRATE JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Janus Kinase (JAK) inhibitor

Direct Interaction yes

Publications:
RGB-286638 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
chembl:CHEMBL2062804 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
PEFICITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
FILGOTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
LS-104 JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Publications:
UPADACITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
ABROCITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
DECERNOTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
OCLACITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
BREPOCITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
SOLCITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

RUXOLITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type hematologic cancer

Response Type decreased response

Approval Status Preclinical

Publications:

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

Hornakova et al., 2011, Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors., Haematologica

Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.

TOFACITINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

ZANUBRUTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

FOSTAMATINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
ENTRECTINIB JAK2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
PEMBROLIZUMAB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type predicted – resistant

Approval Status Clinical Study

Publications:

Zaretsky et al., 2016, Mutations Associated with Acquired Resistance to PD-1 Blockade in Melanoma., N. Engl. J. Med.

SGI-1776 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Indication/Tumor Type bone marrow cancer

Response Type decreased response

Publications:

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

PICTILISIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + Ruxolitinib

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Publications:

Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
PACLITAXEL JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy NVP-BSK805 + paclitaxel

Indication/Tumor Type triple-receptor negative breast cancer

Response Type sensitive

Publications:

Balko et al., 2016, Triple-negative breast cancers with amplification of JAK2 at the 9p24 locus demonstrate JAK2-specific dependence., Sci Transl Med
DACTOLISIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BEZ235 + Ruxolitinib

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Publications:

Choong et al., 2013, Combination treatment for myeloproliferative neoplasms using JAK and pan-class I PI3K inhibitors., J. Cell. Mol. Med.
IMATINIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type myeloid leukemia

Response Type resistant

Approval Status Preclinical - Cell culture

Publications:

Elling et al., 2011, Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease., Blood
LUMINESPIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type decreased response

Publications:

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
ENMD-2076 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ENMD-2076

Novel drug target Novel Target

Publications:
TENALISIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

Publications:
chembl:CHEMBL56543 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Yang SH et al., 2011, Virtual screening and synthesis of quinazolines as novel JAK2 inhibitors., Bioorg Med Chem

CEP-11981 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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

chembl:CHEMBL473773 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TOZASERTIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TRIAMTERENE JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ADAVOSERTIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL379975 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL546797 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL29197 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PF-00562271 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DOVITINIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TYRPHOSTIN 23 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PD-0166285 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ERLOTINIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
LAUROGUADINE JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL1997335 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
GIVINOSTAT JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
AST-487 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL1170485 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
6-AZAURIDINE JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ILORASERTIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
THIRAM JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DASATINIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
GW843682X JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CYC-116 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL71191 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL53898 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CENISERTIB JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TAE-684 JAK2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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:
GuideToPharmacologyGenes: 2048
- Version: 4-March-2015
Alternate Names:

Janus kinase 2 HUGO Gene Name

6192 HUGO Gene ID

JAK2 Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name Janus kinase (JakA) family

GuideToPharmacology Gene Category ID 581

GuideToPharmacology Gene Type enzyme

Gene Categories:

KINASE, TYROSINE KINASE

Publications:

JAX-CKB: JAK2

Version: 15-September-2020

Alternate Names:

3717 CKB Entrez Id

JAK2 CKB Gene Synonym

JTK10 CKB Gene Synonym

Gene Info:

Publications:

Balko et al., 2016, Triple-negative breast cancers with amplification of JAK2 at the 9p24 locus demonstrate JAK2-specific dependence., Sci Transl Med

Weigert et al., 2012, Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition., J. Exp. Med.

Marit et al., 2012, Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor., PLoS ONE

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

DoCM: JAK2

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

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

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.

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

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

CGI: JAK2

Version: 14-September-2020

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

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:
GuideToPharmacologyInteractions: ENSG00000096968
- Version: 20-July-2020
Alternate Names:

Janus kinase 2 GuideToPharmacology Name

O60674 UniProtKB ID

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:
TTD: Janus kinase 2
- Version: 2020.06.01
Alternate Names:

JAK-2 TTD Gene Abbreviation

T08391 TTD Target ID

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:

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:
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:
COSMIC: JAK2
- Version: 4-Sep-2020
Alternate Names:

Gene Info:

Publications:
Oncomine: JAK2
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

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

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	resistant

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

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

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

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

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

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

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

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

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

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

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

3717	Entrez Gene Id
JAK2	Uniprot Gene Name
ENSG00000096968	Ensembl Gene Id

JAK2	DrugBank Gene Name
O60674	UniProt Accession
3717	Entrez Gene Id

JAK-2	UNIPROT
JAK2	GENE_SYMBOL
Tyrosine-protein kinase JAK2	UNIPROT

3717	OncoKB Entrez Id
THCYT3	OncoKB Gene Synonym
JTK10	OncoKB Gene Synonym

JAK2 Gene Record

JAK2 3717 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Nakaya et al., 2011, Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms., Blood Cancer J

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Verstovsek S et al., 2017, A phase 1 study of the Janus kinase 2 (JAK2)<sup>V617F</sup> inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia., Leuk Res

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Purandare AV et al., 2012, Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2., Leukemia

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Genovese MC et al., 2016, Baricitinib in Patients with Refractory Rheumatoid Arthritis., N Engl J Med Kuriya B et al., 2017, Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential., Ther Adv Musculoskelet Dis

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Nakaya et al., 2011, Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms., Blood Cancer J

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type resistant

Publications:

Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Verstovsek S et al., 2017, A phase 1 study of the Janus kinase 2 (JAK2)<sup>V617F</sup> inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia., Leuk Res

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Specific Action of the Ligand Inhibition

Publications:

Purandare AV et al., 2012, Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2., Leukemia

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name lestaurtinib, CEP-701

Novel drug target Novel Target

Indication/Tumor Type hematologic cancer

Publications:

Deshpande et al., 2012, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms., Leukemia

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Response Type resistant

Evidence Type Actionable

Approval Status Preclinical

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Genovese MC et al., 2016, Baricitinib in Patients with Refractory Rheumatoid Arthritis., N Engl J Med

Kuriya B et al., 2017, Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential., Ther Adv Musculoskelet Dis

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Novel Target

Trial Name AC430

Direct Interaction? False

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Janus Kinase (JAK) inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Tyrosine-protein kinase JAK2 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type hematologic cancer

Response Type decreased response

Approval Status Preclinical

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect