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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50194988
Substrate
n/a
Meas. Tech.
ChEMBL_424645 (CHEMBL855706)
IC50
3±n/a nM
Citation
 Hu, Y; Green, N; Gavrin, LK; Janz, K; Kaila, N; Li, HQ; Thomason, JR; Cuozzo, JW; Hall, JP; Hsu, S; Nickerson-Nutter, C; Telliez, JB; Lin, LL; Tam, 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 
Target
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:
MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERSKSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGRYQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVEIQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKGLDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVILCRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPGMRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELPENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
  
Inhibitor
Name:
BDBM50194988
Synonyms:
4-(3-chloro-4-fluorophenylamino)-6-((1,5-dimethyl-1H-imidazol-4-yl)methylamino)quinoline-3-carbonitrile | CHEMBL219682
Type:
Small organic molecule
Emp. Form.:
C22H18ClFN6
Mol. Mass.:
420.87
SMILES:
Cc1c(CNc2ccc3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)ncn1C
Structure:
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