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TargetBromodomain-containing protein 4 [342-460]
LigandBDBM362664
Substrate/Competitorn/a
Meas. Tech.BRD4 AlphaScreen Assay
IC50<25±n/a nM
Citation Combs, APSparks, RB Tricyclic heterocycles as bet protein inhibitors US Patent US10227359 Publication Date 3/12/2019
More Info.:Get all data from this article,  Assay Method
 
Bromodomain-containing protein 4 [342-460]
Name:Bromodomain-containing protein 4 [342-460]
Synonyms:BRD4 | BRD4-BD2 (aa 342-460) | BRD4_HUMAN | Bromodomain containing 4 (aa 342-460) | Bromodomain-containing protein 4 (BRD4)(BD2) | HUNK1
Type:Enzyme Catalytic Domain
Mol. Mass.:13783.81
Organism:Homo sapiens (Human)
Description:a.a. 342-460 (BRD4-BD2)
Residue:119
Sequence:
PAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMS
TIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDE
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM362664
n/a
NameBDBM362664
Synonyms:N-{1-[(4S)-7-(3,5-dimethylisoxazol-4-yl)- 4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4- de][1,4]benzoxazin-2-yl]piperidin-4-yl}-N- methylcyclopropanecarboxamide | US10227359, Example 19 | US9834565, Example 19
TypeSmall organic molecule
Emp. Form.C29H32N6O3
Mol. Mass.512.6028
SMILESCN(C1CCN(CC1)c1nc2ccc(-c3c(C)noc3C)c3OCC(c4ccccn4)n1c23)C(=O)C1CC1 |(-1.35,6.78,;-2.12,5.44,;-1.35,4.11,;-2.12,2.78,;-1.35,1.44,;.19,1.44,;.96,2.78,;.19,4.11,;.96,.11,;2.5,.11,;3.06,-1.33,;4.39,-2.1,;4.39,-3.64,;3.06,-4.41,;3.06,-5.95,;1.81,-6.85,;.35,-6.38,;2.29,-8.32,;3.83,-8.32,;4.3,-6.85,;5.77,-6.38,;1.72,-3.64,;.39,-4.41,;-.94,-3.64,;-.94,-2.1,;-2.28,-1.33,;-3.61,-2.1,;-4.94,-1.33,;-4.94,.21,;-3.61,.98,;-2.28,.21,;.39,-1.33,;1.72,-2.1,;-3.66,5.44,;-4.43,4.11,;-4.43,6.78,;-5.77,7.55,;-4.43,8.32,)|
Structure
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