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Target
Bromodomain-containing protein 4 [342-460]
Ligand
BDBM318524
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:
BDBM318524
Synonyms:
7-(3,5-Dimethylisoxazol-4-yl)-4-ethyl-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one 2,2,2-trifluoroacetate | US10464947, Example 70 | US11498926, Example 70 | US9624241, Example 70
Type:
Small organic molecule
Emp. Form.:
C21H20N4O3
Mol. Mass.:
376.4085
SMILES:
CCC1(COc2c(ccc3[nH]c(=O)n1c23)-c1c(C)noc1C)c1ccccn1 |(.54,4.59,;.94,3.11,;-.15,2.02,;-1.48,1.25,;-1.48,-.29,;-.15,-1.06,;-.15,-2.6,;1.18,-3.37,;2.52,-2.6,;2.52,-1.06,;3.85,-.29,;2.72,1.25,;3.49,2.58,;1.18,1.25,;1.18,-.29,;-1.48,-3.37,;-2.95,-2.9,;-3.72,-1.56,;-3.85,-4.14,;-2.95,-5.39,;-1.48,-4.91,;-.15,-5.68,;-1.24,3.11,;-.84,4.59,;-1.93,5.68,;-3.42,5.28,;-3.81,3.8,;-2.73,2.71,)|
Structure:
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