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Target
Mitogen-activated protein kinase kinase kinase 8
Ligand
BDBM21909
Substrate
Dual specificity mitogen-activated protein kinase kinase 1
Meas. Tech.
Tpl2/Cot Kinase Assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
130±n/a nM
Citation
 Green, N; Hu, Y; Janz, K; Li, HQ; Kaila, N; Guler, S; Thomason, J; Joseph-McCarthy, D; Tam, SY; Hotchandani, R; Wu, J; Huang, A; Wang, Q; Leung, L; Pelker, J; Marusic, S; Hsu, S; Telliez, JB; Hall, JP; Cuozzo, JW; Lin, LL Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles. J Med Chem 50:4728-45 (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:
BDBM21909
Synonyms:
8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-{[2-(1H-imidazol-4-yl)ethyl]amino}quinoline-3-carbonitrile | Cyanoquinoline, 22
Type:
Small organic molecule
Emp. Form.:
C21H15Cl2FN6
Mol. Mass.:
441.288
SMILES:
Fc1ccc(Nc2c(cnc3c(Cl)cc(NCCc4cnc[nH]4)cc23)C#N)cc1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Dual specificity mitogen-activated protein kinase kinase 1
Synonyms:
GST fusion of MAP kinase kinase 1 | GST-MEK1 | MAP2K1 | MEK1 | MP2K1_RABIT | PRKMK1 | glutathione S-transferase-MAP kinase kinase 1
Type:
Other Protein Type
Mol. Mass.:
43453
Organism:
Oryctolagus cuniculus (rabbit)
Description:
Rabbit MEK1 was purchased from Millipore.
Residue:
393
Sequence:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSAVFSLEFQDFVNKCLIKNPAERADLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV