| 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 | BDBM104963 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1613130 (CHEMBL3854930) |
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| IC50 | >25000±n/a nM |
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| Citation |  Glatthar, R; Stojanovic, A; Troxler, T; Mattes, H; Möbitz, H; Beerli, R; Blanz, J; Gassmann, E; Drückes, P; Fendrich, G; Gutmann, S; Martiny-Baron, G; Spence, F; Hornfeld, J; Peel, JE; Sparrer, H Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J Med Chem59:7544-60 (2016) [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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| BDBM104963 |
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| n/a |
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| Name | BDBM104963 |
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| Synonyms: | CHEMBL507361 | US11147816, PD0325901 | US11701360, PD0325901 | US20230270730, Compound ref-1 | US8575391, Q |
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| Type | Small organic molecule |
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| Emp. Form. | C16H14F3IN2O4 |
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| Mol. Mass. | 482.193 |
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| SMILES | OC[C@@H](O)CONC(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F |r| |
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| Structure | 
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