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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318502
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:
BDBM318502
Synonyms:
1-[7-(3,5-Dimethylisoxazol-4-yl)- 4-phenyl-4,5-dihydroimidazo[1,5,4- de][1,4]benzoxazin-2-yl]piperidin- 4-ol | US10464947, Example 57 | US11498926, Example 57 | US9624241, Example 57
Type:
Small organic molecule
Emp. Form.:
C25H26N4O3
Mol. Mass.:
430.4989
SMILES:
Cc1noc(C)c1-c1ccc2nc(N3CCC(O)CC3)n3C(COc1c23)c1ccccc1 |(-.06,-4.94,;1.4,-5.41,;1.88,-6.88,;3.42,-6.88,;3.89,-5.41,;5.36,-4.94,;2.65,-4.51,;2.65,-2.97,;3.98,-2.2,;3.98,-.66,;2.65,.11,;2.08,1.54,;.54,1.54,;-.23,2.88,;-1.77,2.88,;-2.54,4.21,;-1.77,5.55,;-2.54,6.88,;-.23,5.55,;.54,4.21,;-.02,.11,;-1.36,-.66,;-1.36,-2.2,;-.02,-2.97,;1.31,-2.2,;1.31,-.66,;-2.69,.11,;-4.02,-.66,;-5.36,.11,;-5.36,1.65,;-4.02,2.42,;-2.69,1.65,)|
Structure:
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