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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50191774
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1613133
IC50 280±n/a nM
Citation Glatthar RStojanovic ATroxler TMattes HMöbitz HBeerli RBlanz JGassmann EDrückes PFendrich GGutmann SMartiny-Baron GSpence FHornfeld JPeel JESparrer H Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J Med Chem 59:7544-60 (2016) [PubMed]
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 proto-oncogene serine/threonine-protein kinase | Cancer Osaka thyroid oncogene | Mitogen-activated protein kinase kinase kinase 8 | 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:n/a
Residue:467
Sequence:
MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERS
KSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGR
YQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVE
IQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKG
LDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVIL
CRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPG
MRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELP
ENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
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BDBM50191774
n/a
NameBDBM50191774
Synonyms:CHEMBL3899461
TypeSmall organic molecule
Emp. Form.C28H25N7OS
Mol. Mass.507.609
SMILESC(CN1CCOCC1)Nc1nc2ccc(cc2s1)-n1cnc2cnc3cnc(cc3c12)-c1ccccc1
Structure
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