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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM50208911
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1633269 (CHEMBL3876061)
IC50 1262±n/a nM
Citation Katz, JDHaidle, AChilders, KKZabierek, AAJewell, JPHou, YAltman, MDSzewczak, AChen, DHarsch, AHayashi, MWarren, LHutton, MNuthall, HSu, HPMunshi, SStanton, MGDavies, IWMunoz, BNorthrup, A Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. Bioorg Med Chem Lett27:114-120 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase kinase kinase 8
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:
MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERS
KSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGR
YQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVE
IQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKG
LDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVIL
CRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPG
MRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELP
ENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
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  Blast E-value cutoff:
BDBM50208911
n/a
NameBDBM50208911
Synonyms:CHEMBL3884319
TypeSmall organic molecule
Emp. Form.C23H22N4O2
Mol. Mass.386.4464
SMILESCC1(C)C(=O)N([C@H]2CCc3c2cccc3O)c2nc(Nc3ccccc3)ncc12 |r|
Structure
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