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TargetBromodomain-containing protein 4 [1-477]/[333-460]/[44-168]/[44-460]
LigandBDBM331345
Substrate/Competitorn/a
Meas. Tech.Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay
IC50<1±n/a nM
Citation Norris, DJ; Vaccaro, W; DeBenedetto, MV; Degnan, AP; Delucca, GV; Deskus, JA; Han, W; Kumi, GK; Schmitz, WD; Starrett, Jr., JE; Hill, MD; Huang, H Tricyclic compounds as anticancer agents US Patent US9725449 Publication Date 8/8/2017
More Info.:Get all data from this article,  Assay Method
 
Bromodomain-containing protein 4 [1-477]/[333-460]/[44-168]/[44-460]
Name:Bromodomain-containing protein 4 [1-477]/[333-460]/[44-168]/[44-460]
Synonyms:Bromodomain BRD4
Type:Protein
Mol. Mass.:n/a
Description:n/a
Components:This complex has 4 components.
Component 1
Name:Bromodomain-containing protein 4 [44-168]
Synonyms:BET bromodomain 4(1) (BRD4(1)) | BRD4 | BRD4-BD1 protein (aa 44-168) | BRD4_HUMAN | Bromodomain protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4) (aa 44-168) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 bromodomain 1 (BRD4-BD1) | HUNK1
Type:Enzyme Catalytic Domain
Mol. Mass.:14866.49
Organism:Homo sapiens (Human)
Description:aa (44-168)
Residue:125
Sequence:
NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKT
PMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINE
LPTEE
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Component 2
Name:Bromodomain-containing protein 4 [333-460]
Synonyms:BET bromodomain 4(2) (BRD4(2)) | BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 (BRD4) | HUNK1
Type:Enzyme Catalytic Domain
Mol. Mass.:14818.38
Organism:Homo sapiens (Human)
Description:aa (333-460)
Residue:128
Sequence:
KDVPDSQQHPAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCD
IIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEM
RFAKMPDE
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Component 3
Name:Bromodomain-containing protein 4 [1-477]
Synonyms:BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 (BRD4 (aa 1-477) | Bromodomain-containing protein 4 (aa 1-477) | HUNK1
Type:Enzyme Catalytic Domain
Mol. Mass.:53061.90
Organism:Homo sapiens (Human)
Description:aa (1-477)
Residue:477
Sequence:
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQT
NQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYW
NAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRG
RGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMT
VVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTI
DPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGI
LKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGA
DVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPPPT
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Component 4
Name:Bromodomain-containing protein 4 [44-460]
Synonyms:BRD4 | BRD4_HUMAN | Bromodomain-containing protein 4 (BRD4) | HUNK1
Type:Enzyme Catalytic Domain
Mol. Mass.:47039.29
Organism:Homo sapiens (Human)
Description:aa (44-460)
Residue:417
Sequence:
NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKT
PMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINE
LPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPH
PFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVK
TKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPA
PEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTI
KSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDE
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BDBM331345
n/a
NameBDBM331345
Synonyms:1-[5-(Dimethyl-1H-1,2,3-triazol-5-yl)-8-[(S)-oxan-4-yl(phenyl)methyl]-3,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2 | US9725449, Example 179
TypeSmall organic molecule
Emp. Form.C29H31N7O2
Mol. Mass.509.6021
SMILESCc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1nc(ccc21)N1CC(O)C1 |r|
Structure
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