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TargetBromodomain-containing protein 4 [44-477]
LigandBDBM274316
Substrate/Competitorn/a
Meas. Tech.TR-FRET In-Vitro Binding Assay
pH7.5±n/a
IC50 14.0±n/a nM
Commentsextracted
Citation Rueger, HBlank, JBordas, VCotesta, SBold, GGuagnano, VVaupel, A Pyrrolopyrrolone derivatives and their use as BET inhibitors US Patent US9550796 Publication Date 1/24/2017
More Info.:Get all data from this article,  Assay Method
 
Bromodomain-containing protein 4 [44-477]
Name:Bromodomain-containing protein 4 [44-477]
Synonyms:BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 | HUNK1
Type:Enzyme Catalytic Domain (aa 44-477)
Mol. Mass.:48692.13
Organism:Homo sapiens (Human)
Description:O60885[44-477]
Residue:434
Sequence:
NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKT
PMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINE
LPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPH
PFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVK
TKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPA
PEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTI
KSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEE
PVVAVSSPAVPPPT
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  Blast E-value cutoff:
BDBM274316
n/a
NameBDBM274316
Synonyms:3-(1-acetylazetidin-3-yl)-6-(4-chlorophenyl)-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-methyl-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one | US9550796, Example 117
TypeSmall organic molecule
Emp. Form.C26H25ClN6O2
Mol. Mass.488.969
SMILESCC(=O)N1CC(C1)c1cn(C)c2C(N(C(=O)c12)c1cc(C)c2nnc(C)n2c1)c1ccc(Cl)cc1
Structure
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