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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM28039
Substrate
biotin-MEK1-peptide
Meas. Tech.
COT HTRF Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
80±n/a nM
Citation
 Cusack, K; Allen, H; Bischoff, A; Clabbers, A; Dixon, R; Fix-Stenzel, S; Friedman, M; Gaumont, Y; George, D; Gordon, T; Grongsaard, P; Janssen, B; Jia, Y; Moskey, M; Quinn, C; Salmeron, A; Thomas, C; Wallace, G; Wishart, N; Yu, Z Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production. Bioorg Med Chem Lett 19:1722-5 (2009) [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:
BDBM28039
Synonyms:
5-[4-(3-phenylphenyl)thieno[2,3-c]pyridin-2-yl]-1H-1,2,3,4-tetrazole | thieno[2,3-c]pyridine, 4c
Type:
Small organic molecule
Emp. Form.:
C20H13N5S
Mol. Mass.:
355.416
SMILES:
c1c(sc2cncc(-c3cccc(c3)-c3ccccc3)c12)-c1nnn[nH]1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotin-MEK1-peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2380.63
Organism:
n/a
Description:
n/a
Residue:
24
Sequence:
ITINAGAGSGQLIDSMANSFVGTR