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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50194984
Substrate/Competitorn/a
Meas. Tech.ChEMBL_424645 (CHEMBL855706)
IC50 110±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 Lett16:6067-72 (2006) [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
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  Blast E-value cutoff:
BDBM50194984
n/a
NameBDBM50194984
Synonyms:4-(3-chloro-4-fluoro-phenylamino)-6-[(1-oxy-pyridin-2-ylmethyl)-amino]-quinoline-3-carbonitrile | CHEMBL222666
TypeSmall organic molecule
Emp. Form.C22H15ClFN5O
Mol. Mass.419.839
SMILES[O-][n+]1ccccc1CNc1ccc2ncc(C#N)c(Nc3ccc(F)c(Cl)c3)c2c1
Structure
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