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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318657
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:
BDBM318657
Synonyms:
7-(3,5-dimethylisoxazol-4-yl)-N-methyl- 4-pyridin-2-yl-4,5- dihydroimidazo[1,5,4- de][1,4]benzoxazin-2-amine | US10464947, Example 186 | US11498926, Example 186 | US9624241, Example 186
Type:
Small organic molecule
Emp. Form.:
C20H19N5O2
Mol. Mass.:
361.3972
SMILES:
CNc1nc2ccc(-c3c(C)noc3C)c3OCC(c4ccccn4)n1c23 |(-1.77,4.88,;-.23,4.88,;.54,3.55,;2.08,3.55,;2.65,2.11,;3.98,1.34,;3.98,-.2,;2.65,-.97,;2.65,-2.51,;1.4,-3.41,;-.06,-2.94,;1.88,-4.88,;3.42,-4.88,;3.89,-3.41,;5.36,-2.94,;1.31,-.2,;-.02,-.97,;-1.36,-.2,;-1.36,1.34,;-2.69,2.11,;-4.02,1.34,;-5.36,2.11,;-5.36,3.65,;-4.02,4.42,;-2.69,3.65,;-.02,2.11,;1.31,1.34,)|
Structure:
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