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Target Report Card

Target Name and Classification

Target ID CHEMBL2964
Target Type SINGLE PROTEIN
Preferred Name Dual specificity mitogen-activated protein kinase kinase 2
Synonyms Dual specificity mitogen-activated protein kinase kinase 2 | ERK activator kinase 2 | MAP kinase kinase 2 | MAP2K2 | MAPK/ERK kinase 2 | MAPKK 2 | MEK 2 | MEK2 | MKK2 | PRKMK2
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > ste protein kinase group > ste protein kinase ste7 family

Target Components

Component Description Relationship Accession
Dual specificity mitogen-activated protein kinase kinase 2 SINGLE PROTEIN P36507

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111289 Dual specificity mitogen-activated protein kinase kinase; MEK1/2 PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL2105741 TRAMETINIB DIMETHYL SULFOXIDE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 DailyMed FDA
CHEMBL2146883 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 PubMed PubMed
CHEMBL2364607 COBIMETINIB FUMARATE Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 4 DailyMed
CHEMBL1614701 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 PubMed PubMed
CHEMBL3187723 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 3 Other Other PubMed
CHEMBL105442 CI-1040 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 2 PubMed PubMed
CHEMBL507361 PD-0325901 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 2 Other PubMed
CHEMBL2107832 PIMASERTIB Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 2 Other PubMed
CHEMBL2138601 Refametinib Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 2 PubMed
CHEMBL1614766 Ro-4987655 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1 Other PubMed PubMed
CHEMBL1615025 TAK-733 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1 PubMed PubMed
CHEMBL2104954 BALAMAPIMOD Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1 Other
CHEMBL3182621 AZD-8330 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1 Other PubMed
CHEMBL3545081 RG-7304 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1
CHEMBL3545145 WX-554 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1 Other PubMed
CHEMBL3545243 AS-703988 Dual specificity mitogen-activated protein kinase kinase 2 inhibitor 1 Other PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000126934
Ensembl ENSG00000126934
GO Cellular Component GO:0005576 (extracellular region)
GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005769 (early endosome)
GO:0005770 (late endosome)
GO:0005778 (peroxisomal membrane)
GO:0005783 (endoplasmic reticulum)
GO:0005794 (Golgi apparatus)
GO:0005829 (cytosol)
GO:0005874 (microtubule)
GO:0005911 (cell-cell junction)
GO:0005925 (focal adhesion)
GO:0005938 (cell cortex)
GO:0009898 (cytoplasmic side of plasma membrane)
GO:0016020 (membrane)
GO:0048471 (perinuclear region of cytoplasm)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004702 (receptor signaling protein serine/threonine kinase activity)
GO:0004708 (MAP kinase kinase activity)
GO:0004712 (protein serine/threonine/tyrosine kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0030165 (PDZ domain binding)
GO:0032947 (protein complex scaffold)
GO:0043539 (protein serine/threonine kinase activator activity)
GO:0046872 (metal ion binding)
GO:0097110 (scaffold protein binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000187 (activation of MAPK activity)
GO:0001932 (regulation of protein phosphorylation)
GO:0006468 (protein phosphorylation)
GO:0007507 (heart development)
GO:0010629 (negative regulation of gene expression)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0030878 (thyroid gland development)
GO:0032872 (regulation of stress-activated MAPK cascade)
GO:0035897 (proteolysis in other organism)
GO:0036289 (peptidyl-serine autophosphorylation)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0048538 (thymus development)
GO:0048679 (regulation of axon regeneration)
GO:0050772 (positive regulation of axonogenesis)
GO:0060324 (face development)
GO:0060425 (lung morphogenesis)
GO:0060440 (trachea formation)
GO:0060502 (epithelial cell proliferation involved in lung morphogenesis)
GO:0070371 (ERK1 and ERK2 cascade)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071902 (positive regulation of protein serine/threonine kinase activity)
GO:0090170 (regulation of Golgi inheritance)
GO:1903800 (positive regulation of production of miRNAs involved in gene silencing by miRNA)
GO:2000147 (positive regulation of cell motility)
GO:2000641 (regulation of early endosome to late endosome transport)
Wikipedia MAP2K2

Target Cross References - Protein

canSAR P36507
CGD Cardiofaciocutaneous syndrome
Human Protein Atlas ENSG00000126934
IntAct P36507
Guide to Pharmacology 2063
Open Targets ENSG00000126934
PharmGKB PA30587
Pharos P36507 (Tclin)
Reactome R-HSA-112411 (MAPK1 (ERK2) activation.)
R-HSA-445144 (Signal transduction by L1.)
R-HSA-5210891 (Uptake and function of anthrax toxins.)
R-HSA-5673000 (RAF activation.)
R-HSA-5674135 (MAP2K and MAPK activation.)
R-HSA-5674499 (Negative feedback regulation of MAPK pathway.)
R-HSA-6802946 (Signaling by moderate kinase activity BRAF mutants.)
R-HSA-6802948 (Signaling by high-kinase activity BRAF mutants.)
R-HSA-6802949 (Signaling by RAS mutants.)
R-HSA-6802952 (Signaling by BRAF and RAF fusions.)
R-HSA-6802955 (Paradoxical activation of RAF signaling by kinase inactive BRAF.)
UniProt P36507

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR017441 (Protein_kinase_ATP_BS.)
Pfam PF00069 (Pkinase)

Target Cross References - Structure

PDBe 1S9I 4H3Q
CREDO 1S9I 4H3Q
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