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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM419958
Substrate
n/a
Meas. Tech.
AlphaScreen Assay A2
IC50
<100±n/a nM
Citation
 Combs, AP; Sparks, RB; Maduskuie, Jr., TP; Rodgers, JD Tricyclic heterocycles as BET protein inhibitors US Patent  US10464947 Publication Date 11/5/2019 
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:
BDBM419958
Synonyms:
7-(3,5-Dimethylisoxazol-4-yl)-4- phenyl-9-pyridin-3-yl-4,5- dihydroimidazo[1,5,4- de][1,4]benzoxazin-2(1H)-one | US10464947, Example 52
Type:
Small organic molecule
Emp. Form.:
C26H20N4O4
Mol. Mass.:
452.4614
SMILES:
Cc1noc(C)c1-c1cc(C(=O)c2cccnc2)c2[nH]c(=O)n3C(COc1c23)c1ccccc1 |(-.15,-6.16,;-1.48,-5.39,;-2.95,-5.87,;-3.85,-4.62,;-2.95,-3.37,;-3.72,-2.04,;-1.48,-3.85,;-.15,-3.08,;1.18,-3.85,;2.52,-3.08,;3.85,-3.85,;5.19,-3.08,;3.85,-5.39,;2.52,-6.16,;2.52,-7.7,;3.85,-8.47,;5.19,-7.7,;5.19,-6.16,;2.52,-1.54,;3.66,-.51,;3.04,.9,;3.81,2.23,;1.18,.77,;-.15,1.54,;-1.48,.77,;-1.48,-.77,;-.15,-1.54,;1.18,-.77,;-.15,3.08,;-1.48,3.85,;-1.48,5.39,;-.15,6.16,;1.18,5.39,;1.18,3.85,)|
Structure:
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