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Target
Bromodomain-containing protein 4 [342-460]
Ligand
BDBM318480
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 [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:
BDBM318480
Synonyms:
7-(3,5-Dimethylisoxazol-4-yl)-N-methyl-4-phenyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-amine | US10464947, Example 26 | US11498926, Example 26 | US9624241, Example 26
Type:
Small organic molecule
Emp. Form.:
C21H20N4O2
Mol. Mass.:
360.4091
SMILES:
CNc1nc2ccc(-c3c(C)noc3C)c3OCC(c4ccccc4)n1c23 |(4.44,2.1,;2.9,2.1,;2.13,.77,;3.26,-.77,;1.93,-1.54,;1.93,-3.08,;.59,-3.85,;-.74,-3.08,;-2.07,-3.85,;-2.07,-5.39,;-.74,-6.16,;-3.54,-5.87,;-4.44,-4.62,;-3.54,-3.37,;-4.31,-2.04,;-.74,-1.54,;-2.07,-.77,;-2.07,.77,;-.74,1.54,;-.74,3.08,;.59,3.85,;.59,5.39,;-.74,6.16,;-2.07,5.39,;-2.07,3.85,;.59,.77,;.59,-.77,)|
Structure:
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