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TargetDual specificity mitogen-activated protein kinase kinase 1/2
LigandBDBM50099963
Substrate/Competitorn/a
Meas. Tech.ChEMBL_105685 (CHEMBL716467)
IC50 9700±n/a nM
Citation Cockerill, SStubberfield, CStables, JCarter, MGuntrip, SSmith, KMcKeown, SShaw, RTopley, PThomsen, LAffleck, KJowett, AHayes, DWillson, MWoollard, PSpalding, D Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorg Med Chem Lett11:1401-5 (2001) [PubMed]
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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BDBM50099963
n/a
NameBDBM50099963
Synonyms:CHEMBL30432 | N*4*-(1-Benzyl-1H-indazol-5-yl)-N*6*,N*6*-dimethyl-pyrido[3,4-d]pyrimidine-4,6-diamine
TypeSmall organic molecule
Emp. Form.C23H21N7
Mol. Mass.395.4597
SMILESCN(C)c1cc2c(Nc3ccc4n(Cc5ccccc5)ncc4c3)ncnc2cn1
Structure
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