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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50195002
Substrate/Competitorn/a
Meas. Tech.ChEMBL_424645
IC50>40000±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:
BDBM50195002
n/a
NameBDBM50195002
Synonyms:4-(3-chloro-4-fluorophenoxy)-6-(2-morpholinoethylamino)quinoline-3-carbonitrile | CHEMBL222468
TypeSmall organic molecule
Emp. Form.C22H20ClFN4O2
Mol. Mass.426.871
SMILESFc1ccc(Oc2c(cnc3ccc(NCCN4CCOCC4)cc23)C#N)cc1Cl
Structure
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