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TargetBromodomain BRD4
LigandBDBM331207
Substrate/Competitorn/a
Meas. Tech.Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay
IC50<1±n/a nM
Citation Norris DJVaccaro WDeBenedetto MVDegnan APDelucca GVDeskus JAHan WKumi GKSchmitz WDStarrett, Jr. JEHill MDHuang 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 BRD4
Name:Bromodomain BRD4
Synonyms:n/a
Type:Protein
Mol. Mass.:n/a
Description:n/a
Components:This complex has 4 components.
Component 1
Name:Bromodomain-containing protein 4 (BRD4)
Synonyms:BET bromodomain 4(1) (BRD4(1)) | BRD4-BD1 protein (aa 44-168) | Bromodomain protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 (BRD4-BD1) | Bromodomain-containing protein 4 bromodomain 1 (BRD4-BD1)
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 (BRD4)
Synonyms:BET bromodomain 4(2) (BRD4(2))
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 (BRD4)
Synonyms:n/a
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 (BRD4)
Synonyms:n/a
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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BDBM331207
n/a
NameBDBM331207
Synonyms:10-Chloro-5-(dimethyl-1H-1,2,3-triazol-5-yl)-N,N-dimethyl-8-[(S)-oxan-4-yl(phenyl)methyl]-3,8,12-triazatricyclo[7.4.0.02,7]trideca-1(13),2 | US9725449, Example 41
TypeSmall organic molecule
Emp. Form.C28H30ClN7O
Mol. Mass.516.037
SMILESCN(C)c1ncc(Cl)c2n([C@@H](C3CCOCC3)c3ccccc3)c3cc(cnc3c12)-c1c(C)nnn1C |r|
Structure
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