Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 8 |
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Ligand | BDBM28042 |
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Substrate/Competitor | biotin-MEK1-peptide |
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Meas. Tech. | COT HTRF Assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 130±n/a nM |
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Citation | Cusack, K; Allen, H; Bischoff, A; Clabbers, A; Dixon, R; Fix-Stenzel, S; Friedman, M; Gaumont, Y; George, D; Gordon, T; Grongsaard, P; Janssen, B; Jia, Y; Moskey, M; Quinn, C; Salmeron, A; Thomas, C; Wallace, G; Wishart, N; Yu, Z Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production. Bioorg Med Chem Lett19:1722-5 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Mitogen-activated protein kinase kinase kinase 8 |
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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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BDBM28042 |
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biotin-MEK1-peptide |
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Name: | biotin-MEK1-peptide |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2380.63 |
Organism: | n/a |
Description: | n/a |
Residue: | 24 |
Sequence: | biotin-AGAGSGQLIDSMANSFVGTR
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