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Target
Bromodomain-containing protein 4 [342-460]
Ligand
BDBM363500
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
<200±n/a nM
Citation
 Combs, AP; Yue, EW; Maduskuie, 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:
BDBM363500
Synonyms:
9-(3,5-Dimethylisoxazol-4-yl)-6-methoxy-3-pyridin-2-yl-2,3-dihydro[1,4]oxazino[2,3,4-hi]indazole | US9850257, Example 7
Type:
Small organic molecule
Emp. Form.:
C20H18N4O3
Mol. Mass.:
362.3819
SMILES:
COc1nn2C(COc3c(ccc1c23)-c1c(C)noc1C)c1ccccn1 |(3.4,12.23,;3.8,10.74,;2.71,9.65,;.04,9.65,;.04,8.11,;-1.29,7.34,;-1.29,5.8,;.04,5.03,;1.38,5.8,;2.71,5.03,;4.04,5.8,;4.04,7.34,;2.71,8.11,;1.38,7.34,;2.71,3.49,;1.47,2.58,;.13,3.35,;1.94,1.12,;3.48,1.12,;3.96,2.58,;5.29,3.35,;-2.62,8.11,;-2.62,9.65,;-3.96,10.42,;-5.29,9.65,;-5.29,8.11,;-3.96,7.34,)|
Structure:
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