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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318496
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:
BDBM318496
Synonyms:
2-{2-[7-(3,5-Dimethylisoxazol- 4-yl)-2-oxo-1,2,4,5- tetrahydroimidazo[1,5,4- de][1,4]benzoxazin-4- yl]phenoxy}-N-(2- hydroxyethyl)acetamide | US10464947, Example 50 | US11498926, Example 50 | US9624241, Example 50
Type:
Small organic molecule
Emp. Form.:
C24H24N4O6
Mol. Mass.:
464.4706
SMILES:
Cc1noc(C)c1-c1ccc2[nH]c(=O)n3C(COc1c23)c1ccccc1OCC(=O)NCCO |(-.06,-4.63,;1.4,-5.11,;1.88,-6.57,;3.42,-6.57,;3.89,-5.11,;5.36,-4.63,;2.65,-4.21,;2.65,-2.67,;3.98,-1.9,;3.98,-.36,;2.65,.41,;2.08,1.85,;.54,1.85,;-.23,3.18,;-.02,.41,;-1.36,-.36,;-1.36,-1.9,;-.02,-2.67,;1.31,-1.9,;1.31,-.36,;-2.69,.41,;-4.02,-.36,;-5.36,.41,;-5.36,1.95,;-4.02,2.72,;-2.69,1.95,;-1.36,2.72,;-1.36,4.26,;-.02,5.03,;-.02,6.57,;1.31,4.26,;2.65,5.03,;3.98,4.26,;5.31,5.03,)|
Structure:
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