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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50349458
Substrate
n/a
Meas. Tech.
ChEMBL_759415 (CHEMBL1810741)
IC50
4943±n/a nM
Citation
 Hu, Y; Cole, D; Denny, RA; Anderson, DR; Ipek, M; Ni, Y; Wang, X; Thaisrivongs, S; Chamberlain, T; Hall, JP; Liu, J; Luong, M; Lin, LL; Telliez, JB; Gopalsamy, A Discovery of indazoles as inhibitors of Tpl2 kinase. Bioorg Med Chem Lett 21:4758-61 (2011) [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:
BDBM50349458
Synonyms:
CHEMBL1808578
Type:
Small organic molecule
Emp. Form.:
C24H20FN7
Mol. Mass.:
425.4609
SMILES:
CCNCc1cncc(-c2ccc3[nH]nc(-c4nc5cc(C#N)c(F)cc5[nH]4)c3c2)c1C
Structure:
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