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MAP2K2 Gene Record

  • Summary
  • Interactions
  • Claims
  • MAP2K2 5605 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    5605
    MITOGEN-ACTIVATED PROTEIN KINASE KINASE 2
    MAP2K2
    CFC4
    MAPKK2
    MEK2
    MKK2
    PRKMK2
    601263
    6842
    ENSG00000126934
    OTTHUMG00000134286
    P36507
    DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 2
    MP2K2_HUMAN
    ERK activator kinase 2
    MAPK/ERK kinase 2
    MAP kinase kinase 2
    MAPKK 2
    MEK 2
    MEK
    DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 2 (EC 2.7.1.-) (MAP KINASE KINASE 2) (MAPKK 2) (ERK ACTIVATOR KINASE 2) (MAPK/ERK KINASE 2) (MEK2). [SOURCE:UNIPROT/SWISSPROT;ACC:P36507]
    T89055
    4542

    Gene Info:

    Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain
    Human Readable Name DRUGGABLE GENOME
    Interpro Acc IPR002290
    Interpro Short Name Ser/Thr_dual-sp_kinase_dom
    Human Readable Name KINASE
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Uniprot Evidence 1: Evidence at protein level
    Target Class Enzymes
    Target Subclass EC:2.7.12.2
    Gene Biotype PROTEIN_CODING
    (19 More Sources)

    Gene Categories: Category Details

    KINASE
    SERINE THREONINE KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE

    Publications:

    Yeh et al., 2007, Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor., Clin. Cancer Res.
    Dombi et al., 2016, Activity of Selumetinib in Neurofibromatosis Type 1-Related Plexiform Neurofibromas., N. Engl. J. Med.
    Davies et al., 2007, AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models., Mol. Cancer Ther.
    Koelblinger P et al., 2017, A review of binimetinib for the treatment of mutant cutaneous melanoma., Future Oncol
    Salama et al., 2013, Trametinib (GSK1120212) in the treatment of melanoma., Expert Opin Pharmacother
    Long GV et al., 2014, Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma., Nat Commun
    Daouti S et al., 2010, Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models., Mol Cancer Ther
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
  • CHEMBL1956073   MAP2K2

    Interaction Score: 1.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20053779


    Sources:
    DTC

  • COBIMETINIB FUMARATE   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RG-7167   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BALAMAPIMOD   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AZD-8330   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TRAMETINIB DIMETHYL SULFOXIDE   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RG-7304   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AS-703988   MAP2K2

    Interaction Score: 0.77

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PIMASERTIB   MAP2K2

    Interaction Score: 0.69

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Notes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions

  • TAK-733   MAP2K2

    Interaction Score: 0.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions

  • PD-0325901   MAP2K2

    Interaction Score: 0.56

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    23398453


    Sources:
    DTC MyCancerGenome ChemblInteractions

  • COBIMETINIB   MAP2K2

    Interaction Score: 0.55

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial OncoKB

  • ARRY-300   MAP2K2

    Interaction Score: 0.52

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Novel Target
    Trial Name ARRY-300

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • BINIMETINIB   MAP2K2

    Interaction Score: 0.52

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Novel Target
    Trial Name ARRY-162
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

    PMIDs:
    28587477


    Sources:
    MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

  • WX-554   MAP2K2

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name WX-554
    Novel drug target Novel Target
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • REFAMETINIB   MAP2K2

    Interaction Score: 0.44

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • SELUMETINIB   MAP2K2

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    17332304 28029918 17699718


    Sources:
    TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial TTD

  • RG-7420   MAP2K2

    Interaction Score: 0.39

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenome

  • TRAMETINIB   MAP2K2

    Interaction Score: 0.26

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

    Interaction Info:
    Notes

    PMIDs:
    23432625 25452114


    Sources:
    TALC MyCancerGenome ClearityFoundationClinicalTrial CIViC MyCancerGenomeClinicalTrial

  • DABRAFENIB   MAP2K2

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25452114 24265153


    Sources:
    CIViC

  • RO-4987655   MAP2K2

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CI-1040   MAP2K2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    MyCancerGenome ChemblInteractions

  • VEMURAFENIB   MAP2K2

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24265153


    Sources:
    CIViC

  • CHEMBL202721   MAP2K2

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL406845   MAP2K2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL546797   MAP2K2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL379975   MAP2K2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CEDIRANIB   MAP2K2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • JNJ-7706621   MAP2K2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PD-0166285   MAP2K2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • VANDETANIB   MAP2K2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LINIFANIB   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TOZASERTIB   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RG-1530   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DOVITINIB   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TAE-684   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • PF-00562271   MAP2K2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   MAP2K2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   MAP2K2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • Ensembl: ENSG00000126934

    • Version: 101_38

    Alternate Names:
    MAP2K2 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • HopkinsGroom: P36507

    • Version: 11-September-2012

    Alternate Names:
    P36507 Uniprot Accession
    5605 Entrez Gene Id
    ENSG00000126934 Ensembl Gene Id

    Gene Info:
    Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain
    Human Readable Name DRUGGABLE GENOME
    Interpro Acc IPR002290

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • RussLampel: ENSG00000126934

    • Version: 26-July-2011

    Alternate Names:
    DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 2 (EC 2.7.1.-) (MAP KINASE KINASE 2) (MAPKK 2) (ERK ACTIVATOR KINASE 2) (MAPK/ERK KINASE 2) (MEK2). [SOURCE:UNIPROT/SWISSPROT;ACC:P36507] Description
    MAP2K2 Display Id
    ENSG00000126934 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P36507

    • Version: January-2014

    Alternate Names:
    MAP2K2 Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:2.7.12.2

    Publications:

  • CIViC: MAP2K2

    • Version: 14-September-2020

    Alternate Names:
    5605 Entrez Gene ID
    4542 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:
    Long GV et al., 2014, Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma., Nat Commun
    Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov

  • DTC: MAP2K2

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Vasbinder MM et al., 2013, Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors., J Med Chem
    Daouti S et al., 2010, Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models., Mol Cancer Ther

  • HingoraniCasas: ENSG00000126934

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000126934 Gene Symbol
    MAP2K2 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TALC: MEK2

    • Version: 12-May-2016

    Alternate Names:
    MEK2 Gene Symbol

    Gene Info:

    Publications:

  • MyCancerGenome: MAP2K2

    • Version: 20-Jun-2017

    Alternate Names:
    5605 Entrez Gene Id
    MAP2K2 MyCancerGenome Gene Symbol
    MEK MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • ChemblInteractions: MEK2

    • Version: chembl_23

    Alternate Names:
    MKK2 GENE_SYMBOL
    PRKMK2 GENE_SYMBOL
    MAP2K2 GENE_SYMBOL

    Gene Info:

    Publications:

  • OncoKB: MAP2K2

    • Version: 23-July-2020

    Alternate Names:
    5605 OncoKB Entrez Id
    MKK2 OncoKB Gene Synonym
    PRKMK2 OncoKB Gene Synonym

    Gene Info:

    Publications:

  • GO: MAP2K2

    • Version: 01-February-2022

    Alternate Names:
    MEK2 GO Gene Synonym
    MKK2 GO Gene Synonym
    PRKMK2 GO Gene Synonym

    Gene Info:

    Gene Categories:
    SERINE THREONINE KINASE, TYROSINE KINASE

    Publications:

  • Tempus: MAP2K2

    • Version: 11-November-2018

    Alternate Names:
    MAP2K2 Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: MAP2K2

    • Version: 27-Jun-2013

    Alternate Names:
    5605 Gene ID
    MAPKK2 dGene Synonym
    MEK2 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, SERINE THREONINE KINASE

    Publications:

  • TTD: ERK activator kinase 2

    • Version: 2020.06.01

    Alternate Names:
    MEK2 TTD Gene Abbreviation
    T89055 TTD Target ID

    Gene Info:

    Publications:

  • Pharos: MAP2K2

    • Version: 01-February-2022

    Alternate Names:
    Dual specificity mitogen-activated protein kinase kinase 2 Gene Name
    P36507 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE

    Publications:

  • MyCancerGenomeClinicalTrial: MAP2K2

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • ClearityFoundationClinicalTrial: MEK2

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: MAP2K2

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FoundationOneGenes: MAP2K2

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: MAP2K2

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • Oncomine: MAP2K2

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: MAP2K2

    • 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