| Reaction Details |
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 | Report a problem with these data |
| Target | Mitogen-activated protein kinase kinase kinase 8 |
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| Ligand | BDBM50195002 |
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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 |
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| 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 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 52916.89 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P41279 |
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| Residue: | 467 |
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| Sequence: | MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERS
KSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGR
YQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVE
IQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKG
LDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVIL
CRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPG
MRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELP
ENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
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| BDBM50195002 |
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| n/a |
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| Name | BDBM50195002 |
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| Synonyms: | 4-(3-chloro-4-fluorophenoxy)-6-(2-morpholinoethylamino)quinoline-3-carbonitrile | CHEMBL222468 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H20ClFN4O2 |
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| Mol. Mass. | 426.871 |
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| SMILES | Fc1ccc(Oc2c(cnc3ccc(NCCN4CCOCC4)cc23)C#N)cc1Cl |
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| Structure | 
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