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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50307880
Substrate/Competitorn/a
Meas. Tech.ChEMBL_612858 (CHEMBL1067547)
IC50>10000±n/a nM
Citation Nourry, AZambon, ADavies, LNiculescu-Duvaz, IDijkstra, HPMénard, DGaulon, CNiculescu-Duvaz, DSuijkerbuijk, BMFriedlos, FManne, HAKirk, RWhittaker, SMarais, RSpringer, CJ BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. J Med Chem53:1964-78 (2010) [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:
BDBM50307880
n/a
NameBDBM50307880
Synonyms:CHEMBL598626 | N-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yloxy)benzamide
TypeSmall organic molecule
Emp. Form.C27H25N5O3
Mol. Mass.467.5191
SMILESCC(C)(C)c1cc(NC(=O)c2cccc(Oc3cccc4[nH]c(=O)[nH]c34)c2)n(n1)-c1ccccc1
Structure
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