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Target
Bromodomain-containing protein 4 [342-460]
Ligand
BDBM318473
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
<100±n/a nM
Citation
 Combs, AP; Sparks, RB; Maduskuie, Jr., TP Tricyclic heterocycles as BET protein inhibitors US Patent  US9624241 Publication Date 4/18/2017 
Target
Name:
Bromodomain-containing protein 4 [342-460]
Synonyms:
BRD4 | BRD4-BD2 (aa 342-460) | BRD4_HUMAN | Bromodomain containing 4 (aa 342-460) | Bromodomain-containing protein 4 (BRD4)(BD2) | HUNK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
13783.81
Organism:
Homo sapiens (Human)
Description:
a.a. 342-460 (BRD4-BD2)
Residue:
119
Sequence:
PAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDE
  
Inhibitor
Name:
BDBM318473
Synonyms:
7-(3,5-Dimethylisoxazol-4-yl)-4-(tetrahydrofuran-2-yl)-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one | US10464947, Example 18B | US11498926, Example 18A | US9624241, Example 18B
Type:
Small organic molecule
Emp. Form.:
C18H19N3O4
Mol. Mass.:
341.3612
SMILES:
Cc1noc(C)c1-c1ccc2[nH]c(=O)n3[C@@H](COc1c23)C1CCCO1 |r,wU:15.23,(-3.72,-1.69,;-2.95,-3.02,;-3.85,-4.26,;-2.95,-5.51,;-1.48,-5.03,;-.15,-5.8,;-1.48,-3.49,;-.15,-2.72,;1.18,-3.49,;2.52,-2.72,;2.52,-1.18,;3.85,-.41,;2.72,1.13,;3.49,2.46,;1.18,1.13,;-.15,1.9,;-1.48,1.13,;-1.48,-.41,;-.15,-1.18,;1.18,-.41,;-.15,3.44,;1.1,4.34,;.62,5.8,;-.92,5.8,;-1.39,4.34,)|
Structure:
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