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PDBsum entry 5g4r
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Transcription
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PDB id
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5g4r
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References listed in PDB file
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Key reference
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Title
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Gsk6853, A chemical probe for inhibition of the brpf1 bromodomain.
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Authors
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P.Bamborough,
H.A.Barnett,
I.Becher,
M.J.Bird,
C.W.Chung,
P.D.Craggs,
E.H.Demont,
H.Diallo,
D.J.Fallon,
L.J.Gordon,
P.Grandi,
C.I.Hobbs,
E.Hooper-Greenhill,
E.J.Jones,
R.P.Law,
A.Le gall,
D.Lugo,
A.M.Michon,
D.J.Mitchell,
R.K.Prinjha,
R.J.Sheppard,
A.J.Watson,
R.J.Watson.
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Ref.
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Acs Med Chem Lett, 2016,
7,
552-557.
[DOI no: ]
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PubMed id
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Abstract
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The BRPF (Bromodomain and PHD Finger-containing) protein family are important
scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A
selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a
cellular target engagement assay was recently described. Herein, we report the
optimization of this series leading to the identification of a superior BRPF1
inhibitor suitable for in vivo studies.
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