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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318510
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:
BDBM318510
Synonyms:
7-(3,5-Dimethylisoxazol-4-yl)-2-oxo-4-phenyl-1,2,4,5-tetrahydroimidazo[1,5,4-de][1,4]benzoxazine-9-carbonitrile | US10464947, Example 42 | US9624241, Example 42
Type:
Small organic molecule
Emp. Form.:
C21H16N4O3
Mol. Mass.:
372.3767
SMILES:
Cc1noc(C)c1-c1cc(C#N)c2[nH]c(=O)n3C(COc1c23)c1ccccc1 |(-.82,-6.16,;-2.15,-5.39,;-3.61,-5.87,;-4.52,-4.62,;-3.61,-3.37,;-4.38,-2.04,;-2.15,-3.85,;-.82,-3.08,;.52,-3.85,;1.85,-3.08,;3.19,-3.85,;4.52,-4.62,;1.85,-1.54,;3.19,-.77,;2.06,.77,;2.83,2.1,;.52,.77,;-.82,1.54,;-2.15,.77,;-2.15,-.77,;-.82,-1.54,;.52,-.77,;-.82,3.08,;.52,3.85,;.52,5.39,;-.82,6.16,;-2.15,5.39,;-2.15,3.85,)|
Structure:
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