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Target Report Card

Target Name and Classification

Target ID CHEMBL3587
Target Type SINGLE PROTEIN
Preferred Name Dual specificity mitogen-activated protein kinase kinase 1
Synonyms Dual specificity mitogen-activated protein kinase kinase 1 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPKK 1 | MEK 1 | MEK1 | MKK1 | PRKMK1
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 1 SINGLE PROTEIN Q02750

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111289 Dual specificity mitogen-activated protein kinase kinase; MEK1/2 PROTEIN FAMILY
CHEMBL2111351 Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) 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 1 inhibitor 4 DailyMed FDA
CHEMBL2146883 COBIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 PubMed PubMed
CHEMBL2364607 COBIMETINIB FUMARATE Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 4 DailyMed
CHEMBL1614701 SELUMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 PubMed PubMed
CHEMBL3187723 BINIMETINIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 3 Other Other PubMed
CHEMBL105442 CI-1040 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 2 PubMed PubMed
CHEMBL507361 PD-0325901 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 2 Other PubMed
CHEMBL1097999 E-6201 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 2 PubMed PubMed
CHEMBL2107832 PIMASERTIB Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 2 Other PubMed
CHEMBL2138601 Refametinib Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 2 PubMed
CHEMBL1614766 Ro-4987655 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other PubMed PubMed
CHEMBL1615025 TAK-733 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 PubMed PubMed
CHEMBL2104954 BALAMAPIMOD Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other
CHEMBL3182621 AZD-8330 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other PubMed
CHEMBL3330650 RG-7420 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 PubMed
CHEMBL3545081 RG-7304 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 PubMed PubMed PubMed
CHEMBL3545145 WX-554 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other PubMed
CHEMBL3545243 AS-703988 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000169032
Ensembl ENSG00000169032
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005769 (early endosome)
GO:0005770 (late endosome)
GO:0005783 (endoplasmic reticulum)
GO:0005794 (Golgi apparatus)
GO:0005815 (microtubule organizing center)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0005886 (plasma membrane)
GO:0005925 (focal adhesion)
GO:0016020 (membrane)
GO:0070062 (extracellular exosome)
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:0004728 (receptor signaling protein tyrosine phosphatase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008022 (protein C-terminus binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0043539 (protein serine/threonine kinase activator activity)
GO:0047485 (protein N-terminus 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:0006928 (movement of cell or subcellular component)
GO:0006935 (chemotaxis)
GO:0007050 (cell cycle arrest)
GO:0007165 (signal transduction)
GO:0007507 (heart development)
GO:0008285 (negative regulation of cell proliferation)
GO:0010628 (positive regulation of gene expression)
GO:0010629 (negative regulation of gene expression)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0021697 (cerebellar cortex formation)
GO:0030182 (neuron differentiation)
GO:0030216 (keratinocyte differentiation)
GO:0030878 (thyroid gland development)
GO:0032872 (regulation of stress-activated MAPK cascade)
GO:0035897 (proteolysis in other organism)
GO:0045597 (positive regulation of cell differentiation)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0048538 (thymus development)
GO:0048679 (regulation of axon regeneration)
GO:0048870 (cell motility)
GO:0050772 (positive regulation of axonogenesis)
GO:0060020 (Bergmann glial cell differentiation)
GO:0060324 (face development)
GO:0060425 (lung morphogenesis)
GO:0060440 (trachea formation)
GO:0060502 (epithelial cell proliferation involved in lung morphogenesis)
GO:0060674 (placenta blood vessel development)
GO:0060711 (labyrinthine layer development)
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:0090398 (cellular senescence)
GO:0098779 (mitophagy in response to mitochondrial depolarization)
GO:1903800 (positive regulation of production of miRNAs involved in gene silencing by miRNA)
GO:2000641 (regulation of early endosome to late endosome transport)
Wikipedia MAP2K1

Target Cross References - Protein

canSAR Q02750
CGD Cardiofaciocutaneous syndrome
Human Protein Atlas ENSG00000169032
IntAct Q02750
Guide to Pharmacology 2062
Open Targets ENSG00000169032
PharmGKB PA30584
Pharos Q02750 (Tclin)
Reactome R-HSA-110056 (MAPK3 (ERK1) 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-5684264 (MAP3K8 (TPL2)-dependent MAPK1/3 activation.)
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 Q02750

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 1S9J 2P55 3DV3 3DY7 3E8N 3EQB 3EQC 3EQD 3EQF 3EQG 3EQH 3EQI 3MBL 3ORN 3OS3 3PP1 3SLS 3V01 3V04 3VVH 3W8Q 3WIG 3ZLS 3ZLW More...
CREDO 1S9J 2P55 3DV3 3DY7 3E8N 3EQB 3EQC 3EQD 3EQF 3EQG 3EQH 3EQI 3MBL 3ORN 3OS3 3PP1 3SLS 3V01 3V04 3VVH 3W8Q 3WIG 3ZLS 3ZLW More...
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