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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318532
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:
BDBM318532
Synonyms:
7-(3,5-dimethylisoxazol-4-yl)- 4-(5-fluoropyridin-3-yl)-4,5- dihydroimidazo[1,5,4- de][1,4]benzoxazin-2(1H)-one | US10464947, Example 78 | US11498926, Example 78 | US9624241, Example 78
Type:
Small organic molecule
Emp. Form.:
C19H15FN4O3
Mol. Mass.:
366.3458
SMILES:
Cc1noc(C)c1-c1ccc2[nH]c(=O)n3C(COc1c23)c1cncc(F)c1 |(.6,-2.94,;2.07,-3.41,;2.54,-4.88,;4.08,-4.88,;4.56,-3.41,;6.02,-2.94,;3.31,-2.51,;3.31,-.97,;4.65,-.2,;4.65,1.34,;3.31,2.11,;2.75,3.55,;1.21,3.55,;.44,4.88,;.65,2.11,;-.69,1.34,;-.69,-.2,;.65,-.97,;1.98,-.2,;1.98,1.34,;-2.02,2.11,;-2.02,3.65,;-3.36,4.42,;-4.69,3.65,;-4.69,2.11,;-6.02,1.34,;-3.36,1.34,)|
Structure:
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