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Target
Bromodomain-containing protein 4 [368-440]
Ligand
BDBM249283
Substrate
n/a
Meas. Tech.
HTRF Assay
IC50
54.4±n/a nM
Citation
 Aktoudianakis, E; Chin, G; Corkey, BK; Du, J; Elbel, K; Jiang, RH; Kobayashi, T; Lee, R; Martinez, R; Metobo, SE; Mish, M; Munoz, M; Shevick, S; Sperandio, D; Yang, H; Zablocki, J Benzimidazole derivatives as bromodomain inhibitors US Patent  US10017501 Publication Date 7/10/2018 
Target
Name:
Bromodomain-containing protein 4 [368-440]
Synonyms:
BRD4 | BRD4_HUMAN | Bromo domain 2 | Bromodomain-containing protein 4 (BD2) | Bromodomain-containing protein 4 (BRD4) Bromo 2 | Bromodomain-containing protein 4 (BRD4)(BD2) | Bromodomain-containing protein 4 (BRD4)(Bromo 2) | Bromodomain-containing protein 4 Bromo 2 domain(BRD4 BD2) | Bromodomain-containing protein 4 Bromodomain 2 (BRD4-2) | Bromodomain-containing protein 4 Domain 2 | HUNK1
Type:
Protein
Mol. Mass.:
8564.63
Organism:
Homo sapiens (Human)
Description:
BD2 (368-440 aa) of O60885
Residue:
73
Sequence:
KHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVV
  
Inhibitor
Name:
BDBM249283
Synonyms:
US10017501, Compound 1020-57 | US9458145, 1020-57
Type:
Small organic molecule
Emp. Form.:
C22H22N4O
Mol. Mass.:
358.4363
SMILES:
Cc1noc(C)c1-c1cc(-c2c(C)ccnc2C)c2[nH]c(nc2c1)C1CC1 |(1.89,3.53,;.56,4.3,;.08,5.77,;-1.46,5.77,;-1.94,4.3,;-3.27,3.53,;-.69,3.4,;-.69,1.86,;.64,1.09,;.64,-.45,;1.98,-1.22,;1.98,-2.76,;.64,-3.53,;3.31,-3.53,;4.65,-2.76,;4.65,-1.22,;3.31,-.45,;3.31,1.09,;-.69,-1.22,;-1.01,-2.73,;-2.54,-2.89,;-3.17,-1.48,;-2.02,-.45,;-2.02,1.09,;-3.31,-4.23,;-4.65,-5,;-3.31,-5.77,)|
Structure:
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