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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM362664
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
<25±n/a nM
Citation
 Combs, AP; Sparks, RB Tricyclic heterocycles as bet protein inhibitors US Patent  US9834565 Publication Date 12/5/2017 
Target
Name:
Bromodomain-containing protein 4 [42-168]
Synonyms:
BRD4 | BRD4 BD1 (aa 42-168) | BRD4_HUMAN | Bromodomain-containing protein 4 Bromo Domain 1 | HUNK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
15054.68
Organism:
Homo sapiens (Human)
Description:
O60885[42-168]
Residue:
127
Sequence:
STNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE
  
Inhibitor
Name:
BDBM362664
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
Type:
Small organic molecule
Emp. Form.:
C29H32N6O3
Mol. Mass.:
512.6028
SMILES:
CN(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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