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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM21898
Substrate
n/a
Meas. Tech.
ChEMBL_529509 (CHEMBL966653)
IC50
12±n/a nM
Citation
 Hall, JP; Kurdi, Y; Hsu, S; Cuozzo, J; Liu, J; Telliez, JB; Seidl, KJ; Winkler, A; Hu, Y; Green, N; Askew, GR; Tam, S; Clark, JD; Lin, LL Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. J Biol Chem 282:33295-304 (2007) [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:
BDBM21898
Synonyms:
8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[(1H-imidazol-4-ylmethyl)amino]quinoline-3-carbonitrile | CHEMBL436817 | Cyanoquinoline, 11
Type:
Small organic molecule
Emp. Form.:
C20H13Cl2FN6
Mol. Mass.:
427.262
SMILES:
Fc1ccc(Nc2c(cnc3c(Cl)cc(NCc4cnc[nH]4)cc23)C#N)cc1Cl
Structure:
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