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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50194981
Substrate/Competitorn/a
Meas. Tech.ChEMBL_424645
IC50 210±n/a nM
Citation Hu YGreen NGavrin LKJanz KKaila NLi HQThomason JRCuozzo JWHall JPHsu SNickerson-Nutter CTelliez JBLin LLTam S Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett 16:6067-72 (2006) [PubMed]  Article
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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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  Blast E-value cutoff:
BDBM50194981
n/a
NameBDBM50194981
Synonyms:6-(benzylamino)-4-(3-chloro-4-fluorophenylamino)quinoline-3-carbonitrile | CHEMBL373480
TypeSmall organic molecule
Emp. Form.C23H16ClFN4
Mol. Mass.402.851
SMILESFc1ccc(Nc2c(cnc3ccc(NCc4ccccc4)cc23)C#N)cc1Cl
Structure
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