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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50243761
Substrate/Competitorn/a
Meas. Tech.ChEMBL_555010 (CHEMBL957985)
IC50 32000±n/a nM
Citation Peifer, CSelig, RKinkel, KOtt, DTotzke, FSchächtele, CHeidenreich, RRöcken, MSchollmeyer, DLaufer, S Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. J Med Chem51:3814-24 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase kinase kinase 8
Name:Mitogen-activated protein kinase kinase kinase 8
Synonyms:C-COT | COT | COT proto-oncogene serine/threonine-protein kinase | Cancer Osaka thyroid oncogene | ESTF | M3K8_HUMAN | MAP3K8 | Tpl-2 | Tumor Progression Loci-2 Kinase (COT) | Tumor progression locus 2
Type:Serine/threonine-protein kinase
Mol. Mass.:52916.89
Organism:Homo sapiens (Human)
Description:P41279
Residue:467
Sequence:
MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERS
KSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGR
YQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVE
IQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKG
LDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVIL
CRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPG
MRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELP
ENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50243761
n/a
NameBDBM50243761
Synonyms:4-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1,5-dihydro-2H-pyrrole-2-one | CHEMBL529663
TypeSmall organic molecule
Emp. Form.C21H20N2O4
Mol. Mass.364.3945
SMILESCOc1cc(cc(OC)c1OC)C1=C(CNC1=O)c1c[nH]c2ccccc12 |t:13|
Structure
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