Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM50173834
Substrate
n/a
Meas. Tech.
ChEMBL_529509 (CHEMBL966653)
IC50
16±n/a nM
Citation
 Hall, JP; Kurdi, Y; Hsu, S; Cuozzo, J; Liu, J; Telliez, JB; Seidl, KJ; Winkler, A; Hu, Y; Green, N; Askew, GR; Tam, S; Clark, JD; Lin, LL Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood. J Biol Chem 282:33295-304 (2007) [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:
BDBM50173834
Synonyms:
(R)-4-(3-chloro-4-fluorophenylamino)-6-(1-phenylethylamino)-1,7-naphthyridine-3-carbonitrile | CHEMBL199230
Type:
Small organic molecule
Emp. Form.:
C23H17ClFN5
Mol. Mass.:
417.866
SMILES:
C[C@@H](Nc1cc2c(Nc3ccc(F)c(Cl)c3)c(cnc2cn1)C#N)c1ccccc1 |r|
Structure:
Search PDB for entries with ligand similarity: