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Target
Bromodomain-containing protein 4 [368-440]
Ligand
BDBM249284
Substrate
n/a
Meas. Tech.
HTRF Assay
IC50
69.1±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:
BDBM249284
Synonyms:
US10017501, Compound 1020-72 | US9458145, 1020-72
Type:
Small organic molecule
Emp. Form.:
C21H23N5O
Mol. Mass.:
361.4402
SMILES:
Cc1n[nH]c(C)c1-c1cc(cc2nc(C3CC3)n(C)c12)-c1c(C)noc1C |(4.36,.59,;3.59,-.75,;4.5,-1.99,;3.59,-3.24,;2.13,-2.76,;.79,-3.53,;2.13,-1.22,;.79,-.45,;.79,1.09,;-.54,1.86,;-1.87,1.09,;-1.87,-.45,;-3.02,-1.48,;-2.39,-2.89,;-3.16,-4.23,;-4.5,-5,;-3.16,-5.77,;-.86,-2.73,;.23,-3.82,;-.54,-1.22,;-.54,3.4,;-1.79,4.3,;-3.12,3.53,;-1.31,5.77,;.23,5.77,;.71,4.3,;2.04,3.53,)|
Structure:
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