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ChEMBL Statistics
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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
CHEMBL2111351 Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) PROTEIN FAMILY
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 1 inhibitor 4 DailyMed
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
CHEMBL1615025 TAK-733 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 PubMed
CHEMBL3182621 AZD-8330 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other
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
CHEMBL3545243 AS-703988 Dual specificity mitogen-activated protein kinase kinase 1 inhibitor 1 Other
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:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO Molecular Function GO:0004674 (protein serine/threonine kinase activity)
GO:0004708 (MAP kinase kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0005524 (ATP binding)
GO Biological Process GO:0000186 (activation of MAPKK activity)
GO:0000187 (activation of MAPK activity)
GO:0002755 (MyD88-dependent toll-like receptor signaling pathway)
GO:0002756 (MyD88-independent toll-like receptor signaling pathway)
GO:0007050 (cell cycle arrest)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0007265 (Ras protein signal transduction)
GO:0007411 (axon guidance)
GO:0008063 (Toll signaling pathway)
GO:0008285 (negative regulation of cell proliferation)
GO:0008286 (insulin receptor signaling pathway)
GO:0034130 (toll-like receptor 1 signaling pathway)
GO:0034134 (toll-like receptor 2 signaling pathway)
GO:0034138 (toll-like receptor 3 signaling pathway)
GO:0034142 (toll-like receptor 4 signaling pathway)
GO:0045087 (innate immune response)
GO:0048011 (nerve growth factor receptor signaling pathway)
GO:0051403 (stress-activated MAPK cascade)
GO:0090398 (cellular senescence)
Wikipedia MAP2K1

Target Cross References - Protein

canSAR Q02750
CGD Cardiofaciocutaneous syndrome
Human Protein Atlas ENSG00000169032
IntAct Q02750
Guide to Pharmacology 2062 (mitogen-activated protein kinase kinase 1)
PharmGKB PA30584
Reactome REACT_11061 (Signalling by NGF.)
REACT_16888 (Signaling by PDGF.)
REACT_18266 (Axon guidance.)
REACT_498 (Signaling by Insulin receptor.)
REACT_6900 (Signaling in Immune system.)
REACT_9417 (Signaling by EGFR.)
UniProt Q02750

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_cat_dom.)
IPR002290 (Ser/Thr_prot_kinase_dom.)
IPR008271 (Ser/Thr_prot_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR017442 (Se/Thr_prot_kinase-like_dom.)
Pfam PF00069 (Pkinase)

Target Cross References - Structure

PDBe 1S9J 2P55 3DV3 3DY7 3E8N 3EQB 3EQC 3EQD 3EQF 3EQG 3EQH 3EQI 3MBL 3ORN 3PP1
CREDO 1S9J 2P55 3DV3 3DY7 3E8N 3EQB 3EQC 3EQD 3EQF 3EQG 3EQH 3EQI 3MBL 3ORN 3PP1
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