Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50349476
Substrate
n/a
Meas. Tech.
ChEMBL_759415 (CHEMBL1810741)
IC50
>100000±n/a nM
Citation
 Hu, YCole, DDenny, RAAnderson, DRIpek, MNi, YWang, XThaisrivongs, SChamberlain, THall, JPLiu, JLuong, MLin, LLTelliez, JBGopalsamy, 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:
BDBM50349476
Synonyms:
CHEMBL1808596
Type:
Small organic molecule
Emp. Form.:
C25H24N6O
Mol. Mass.:
424.4977
SMILES:
Cc1c(CN2CCOCC2)cncc1-c1ccc2[nH]nc(-c3nc4ccccc4[nH]3)c2c1
Structure:
Search PDB for entries with ligand similarity: