Target
Bromodomain-containing protein 4 [342-460]
Ligand
BDBM363502
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
<200±n/a nM
Citation
 Combs, APYue, EWMaduskuie, TP Tricyclic heterocycles as BET protein inhibitors US Patent  US9850257 Publication Date 12/26/2017 
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:
BDBM363502
Synonyms:
US9850257, Example 9
Type:
Small organic molecule
Emp. Form.:
C20H16BrN3O2
Mol. Mass.:
410.264
SMILES:
Cc1noc(C)c1-c1cc(Br)c2cnn3C(COc1c23)c1ccccc1 |(.09,-2.42,;1.42,-3.19,;1.9,-4.65,;3.44,-4.65,;3.91,-3.19,;5.25,-2.42,;2.67,-2.28,;2.67,-.74,;4,.03,;4,1.57,;5.33,2.34,;2.67,2.34,;2.67,3.88,;,3.88,;,2.34,;-1.33,1.57,;-1.33,.03,;,-.74,;1.33,.03,;1.33,1.57,;-2.67,2.34,;-2.67,3.88,;-4,4.65,;-5.33,3.88,;-5.33,2.34,;-4,1.57,)|
Structure:
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