Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50191944
Substrate
n/a
Meas. Tech.
ChEMBL_1613130 (CHEMBL3854930)
IC50
1300±n/a nM
Citation
 Glatthar, RStojanovic, ATroxler, TMattes, HMöbitz, HBeerli, RBlanz, JGassmann, EDrückes, PFendrich, GGutmann, SMartiny-Baron, GSpence, FHornfeld, JPeel, JESparrer, H Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J Med Chem 59:7544-60 (2016) [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:
BDBM50191944
Synonyms:
CHEMBL3987154
Type:
Small organic molecule
Emp. Form.:
C23H16N6
Mol. Mass.:
376.4133
SMILES:
Cc1ccc(cc1)-c1cc2c3n(cnc3cnc2cn1)-c1ccc2nc[nH]c2c1
Structure:
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