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TargetDual specificity mitogen-activated protein kinase kinase 1/2
LigandBDBM50209763
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1633954 (CHEMBL3876746)
IC50 400±n/a nM
Citation Wu, WChordia, MDHart, BPKumarasinghe, ESJi, MKBhargava, ALawlor, MWShin, JYSera, FHomma, SMuchir, AKhire, URWorman, HJ Macrocyclic MEK1/2 inhibitor with efficacy in a mouse model of cardiomyopathy caused by lamin A/C gene mutation. Bioorg Med Chem25:1004-1013 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Dual specificity mitogen-activated protein kinase kinase 1/2
Name:Dual specificity mitogen-activated protein kinase kinase 1/2
Synonyms:Dual specificity mitogen-activated protein kinase kinase; MEK1/2 | p-MEK1/2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 795758
Components:This complex has 2 components.
Component 1
Name:Dual specificity mitogen-activated protein kinase kinase 2
Synonyms:Dual specificity mitogen-activated protein kinase kinase 2 (MEK2) | Dual specificity mitogen-activated protein kinase kinase; MEK1/2 | ERK activator kinase 2 | MAP kinase kinase 2 | MAP2K2 | MAPK/ERK kinase 2 | MAPKK 2 | MEK2 | MKK2 | MP2K2_HUMAN | PRKMK2 | VHL-MAP2K1/MAP2K2
Type:Enzyme Catalytic Domain
Mol. Mass.:44423.61
Organism:Homo sapiens (Human)
Description:gi_13489054
Residue:400
Sequence:
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQ
KAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQ
VLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRG
LAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQ
GTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRP
PGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADL
KMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV
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Component 2
Name:Dual specificity mitogen-activated protein kinase kinase 1
Synonyms:Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | MEK1 | MP2K1_HUMAN | Mitogen-activated protein kinase 1 (MEK1) | PRKMK1 | VHL-MAP2K1/MAP2K2
Type:Other Protein Type
Mol. Mass.:43439.03
Organism:Homo sapiens (Human)
Description:Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates.
Residue:393
Sequence:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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BDBM50209763
n/a
NameBDBM50209763
Synonyms:CHEMBL3883792
TypeSmall organic molecule
Emp. Form.C19H18F3IN2O5S
Mol. Mass.570.321
SMILESOC1COc2cc(F)c(F)c(Nc3ccc(I)cc3F)c2NS(=O)(=O)C2(CC2)CC1O
Structure
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