Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50264866
Substrate
n/a
Meas. Tech.
ChEMBL_496717 (CHEMBL1005354)
IC50
10±n/a nM
Citation
 George, DFriedman, MAllen, HArgiriadi, MBarberis, CBischoff, AClabbers, ACusack, KDixon, RFix-Stenzel, SGordon, TJanssen, BJia, YMoskey, MQuinn, CSalmeron, JAWishart, NWoller, KYu, Z Discovery of thieno[2,3-c]pyridines as potent COT inhibitors. Bioorg Med Chem Lett 18:4952-5 (2008) [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:
BDBM50264866
Synonyms:
4'-(2-(2H-tetrazol-5-yl)thieno[2,3-c]pyridin-4-yloxy)biphenyl-4-carboxamide | CHEMBL491228
Type:
Small organic molecule
Emp. Form.:
C21H14N6O2S
Mol. Mass.:
414.44
SMILES:
NC(=O)c1ccc(cc1)-c1ccc(Oc2cncc3sc(cc23)-c2nnn[nH]2)cc1
Structure:
Search PDB for entries with ligand similarity: