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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318505
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:
BDBM318505
Synonyms:
4-[7-(3,5-Dimethylisoxazol-4-yl)- 4-phenyl-4,5-dihydroimidazo[1,5,4- de][1,4]benzoxazin-2-yl]piperazine- 1-carboxylate | US10464947, Example 60 | US11498926, Example 60 | US9624241, Example 60
Type:
Small organic molecule
Emp. Form.:
C25H24N5O4
Mol. Mass.:
458.4897
SMILES:
Cc1noc(C)c1-c1ccc2nc(N3CCN(CC3)C([O-])=O)n3C(COc1c23)c1ccccc1 |(-.06,-5.61,;1.4,-6.08,;1.88,-7.55,;3.42,-7.55,;3.89,-6.08,;5.36,-5.61,;2.65,-5.18,;2.65,-3.64,;3.98,-2.87,;3.98,-1.33,;2.65,-.56,;2.08,.88,;.54,.88,;-.23,2.21,;.54,3.55,;-.23,4.88,;-1.77,4.88,;-2.54,3.55,;-1.77,2.21,;-2.54,6.21,;-4.08,6.21,;-1.77,7.55,;-.02,-.56,;-1.36,-1.33,;-1.36,-2.87,;-.02,-3.64,;1.31,-2.87,;1.31,-1.33,;-2.69,-.56,;-4.02,-1.33,;-5.36,-.56,;-5.36,.98,;-4.02,1.75,;-2.69,.98,)|
Structure:
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