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Target
Bromodomain-containing protein 4 [42-168]
Ligand
BDBM318485
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:
BDBM318485
Synonyms:
2-{[7-(3,5-Dimethylisoxazol-4-yl)-4-phenyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl]amino}propan-1-ol | US10464947, Example 31 | US9624241, Example 31
Type:
Small organic molecule
Emp. Form.:
C23H24N4O3
Mol. Mass.:
404.4617
SMILES:
CC(CO)Nc1nc2ccc(-c3c(C)noc3C)c3OC[C@@H](c4ccccc4)n1c23 |r,wU:21.22,(4.06,.77,;3.29,2.1,;4.06,3.44,;5.6,3.44,;1.75,2.1,;.98,.77,;2.11,-.77,;.77,-1.54,;.77,-3.08,;-.56,-3.85,;-1.9,-3.08,;-3.23,-3.85,;-3.23,-5.39,;-1.9,-6.16,;-4.69,-5.87,;-5.6,-4.62,;-4.69,-3.37,;-5.46,-2.04,;-1.9,-1.54,;-3.23,-.77,;-3.23,.77,;-1.9,1.54,;-1.9,3.08,;-.56,3.85,;-.56,5.39,;-1.9,6.16,;-3.23,5.39,;-3.23,3.85,;-.56,.77,;-.56,-.77,)|
Structure:
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