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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50173839
Substrate
n/a
Meas. Tech.
ChEMBL_326807 (CHEMBL860389)
IC50
>40000±n/a nM
Citation
 Gavrin, LK; Green, N; Hu, Y; Janz, K; Kaila, N; Li, HQ; Tam, SY; Thomason, JR; Gopalsamy, A; Ciszewski, G; Cuozzo, JW; Hall, JP; Hsu, S; Telliez, JB; Lin, LL Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg Med Chem Lett 15:5288-92 (2005) [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:
BDBM50173839
Synonyms:
6-(benzyl(methyl)amino)-4-(3-chloro-4-fluorophenylamino)-1,7-naphthyridine-3-carbonitrile | CHEMBL198647
Type:
Small organic molecule
Emp. Form.:
C23H17ClFN5
Mol. Mass.:
417.866
SMILES:
CN(Cc1ccccc1)c1cc2c(Nc3ccc(F)c(Cl)c3)c(cnc2cn1)C#N
Structure:
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