Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 8 |
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Ligand | BDBM50195013 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_424645 (CHEMBL855706) |
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IC50 | >40000±n/a nM |
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Citation | Hu, Y; Green, N; Gavrin, LK; Janz, K; Kaila, N; Li, HQ; Thomason, JR; Cuozzo, JW; Hall, JP; Hsu, S; Nickerson-Nutter, C; Telliez, JB; Lin, LL; Tam, S Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett16:6067-72 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50195013 |
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n/a |
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Name | BDBM50195013 |
Synonyms: | 6-((1H-imidazol-4-yl)methylamino)-4-(3-chloro-4-fluorophenylamino)-7-(trifluoromethoxy)quinoline-3-carbonitrile | CHEMBL374258 |
Type | Small organic molecule |
Emp. Form. | C21H13ClF4N6O |
Mol. Mass. | 476.814 |
SMILES | Fc1ccc(Nc2c(cnc3cc(OC(F)(F)F)c(NCc4cnc[nH]4)cc23)C#N)cc1Cl |
Structure |
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