Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 8 |
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Ligand | BDBM50243761 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_555010 (CHEMBL957985) |
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IC50 | 32000±n/a nM |
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Citation | Peifer, C; Selig, R; Kinkel, K; Ott, D; Totzke, F; Schächtele, C; Heidenreich, R; Röcken, M; Schollmeyer, D; Laufer, S Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. J Med Chem51:3814-24 (2008) [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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BDBM50243761 |
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n/a |
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Name | BDBM50243761 |
Synonyms: | 4-(1H-Indol-3-yl)-3-(3,4,5-trimethoxyphenyl)-1,5-dihydro-2H-pyrrole-2-one | CHEMBL529663 |
Type | Small organic molecule |
Emp. Form. | C21H20N2O4 |
Mol. Mass. | 364.3945 |
SMILES | COc1cc(cc(OC)c1OC)C1=C(CNC1=O)c1c[nH]c2ccccc12 |t:13| |
Structure |
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