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TargetBromodomain-containing protein 4 [342-460]
LigandBDBM362659
Substrate/Competitorn/a
Meas. Tech.AlphaScreen Assay
IC50<25±n/a nM
Citation Combs, APSparks, RB Tricyclic heterocycles as bet protein inhibitors US Patent US9834565 Publication Date 12/5/2017
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:
BDBM362659
n/a
NameBDBM362659
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}ethanesulfonamide | US10227359, Example 14 | US9834565, Example 14
TypeSmall organic molecule
Emp. Form.C26H30N6O4S
Mol. Mass.522.619
SMILESCCS(=O)(=O)NC1CCN(CC1)c1nc2ccc(-c3c(C)noc3C)c3OCC(c4ccccn4)n1c23 |(-5.87,7.44,;-5.1,6.11,;-3.56,6.11,;-3.56,7.65,;-3.56,4.57,;-2.02,6.11,;-1.25,4.78,;-2.02,3.44,;-1.25,2.11,;.29,2.11,;1.06,3.44,;.29,4.78,;1.06,.77,;2.6,.77,;3.16,-.66,;4.49,-1.43,;4.49,-2.97,;3.16,-3.74,;3.16,-5.28,;1.91,-6.18,;.45,-5.71,;2.39,-7.65,;3.93,-7.65,;4.41,-6.18,;5.87,-5.71,;1.83,-2.97,;.49,-3.74,;-.84,-2.97,;-.84,-1.43,;-2.17,-.66,;-3.51,-1.43,;-4.84,-.66,;-4.84,.88,;-3.51,1.65,;-2.17,.88,;.49,-.66,;1.83,-1.43,)|
Structure
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