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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50175241
Substrate
n/a
Meas. Tech.
ChEMBL_328344 (CHEMBL864559)
IC50
>20000±n/a nM
Citation
 Akritopoulou-Zanze, I; Darczak, D; Sarris, K; Phelan, KM; Huth, JR; Song, D; Johnson, EF; Jia, Y; Djuric, SW Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors. Bioorg Med Chem Lett 16:96-9 (2005) [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:
BDBM50175241
Synonyms:
CHEMBL199383 | N-(4-methoxybenzyl)-3-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxamide
Type:
Small organic molecule
Emp. Form.:
C20H17N3O2S
Mol. Mass.:
363.433
SMILES:
COc1ccc(CNC(=O)c2cc3c(n[nH]c3s2)-c2ccccc2)cc1
Structure:
Search PDB for entries with ligand similarity: