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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50307878
Substrate
n/a
Meas. Tech.
ChEMBL_612858 (CHEMBL1067547)
IC50
>10000±n/a nM
Citation
 Nourry, A; Zambon, A; Davies, L; Niculescu-Duvaz, I; Dijkstra, HP; Ménard, D; Gaulon, C; Niculescu-Duvaz, D; Suijkerbuijk, BM; Friedlos, F; Manne, HA; Kirk, R; Whittaker, S; Marais, R; Springer, CJ BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. J Med Chem 53:1964-78 (2010) [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:
BDBM50307878
Synonyms:
1-(3-Tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(3-(2-oxo-2,3-dihydro-1Himidazo[4,5-b]pyridin-7-yloxy)phenyl)urea | CHEMBL597592
Type:
Small organic molecule
Emp. Form.:
C27H26N6O3
Mol. Mass.:
482.5337
SMILES:
CC(C)(C)c1cc(NC(=O)Nc2cccc(Oc3cccc4[nH]c(=O)[nH]c34)c2)n(n1)-c1ccccc1
Structure:
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