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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318504
Substrate
n/a
Meas. Tech.
AlphaScreen Assay A1
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:
BDBM318504
Synonyms:
1-[7-(3,5-Dimethylisoxazol-4-yl)- 4-phenyl-4,5-dihydroimidazo[1,5,4- de][1,4]benzoxazin-2-yl]azetidin- 3-ol | US10464947, Example 59 | US11498926, Example 59 | US9624241, Example 59
Type:
Small organic molecule
Emp. Form.:
C23H22N4O3
Mol. Mass.:
402.4458
SMILES:
Cc1noc(C)c1-c1ccc2nc(N3CC(O)C3)n3C(COc1c23)c1ccccc1 |(-.06,-4.55,;1.4,-5.02,;1.88,-6.49,;3.42,-6.49,;3.89,-5.02,;5.36,-4.55,;2.65,-4.12,;2.65,-2.58,;3.98,-1.81,;3.98,-.27,;2.65,.5,;2.08,1.94,;.54,1.94,;-.23,3.27,;-1.72,3.67,;-1.32,5.15,;-2.09,6.49,;.17,4.76,;-.02,.5,;-1.36,-.27,;-1.36,-1.81,;-.02,-2.58,;1.31,-1.81,;1.31,-.27,;-2.69,.5,;-4.02,-.27,;-5.36,.5,;-5.36,2.04,;-4.02,2.81,;-2.69,2.04,)|
Structure:
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