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6TQ2

N-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 5-(4-(4-fluorophenyl)-1H-imidazol-5-yl)-1-methylpyridin-2(1H)-one

This is a non-PDB format compatible entry.
Summary for 6TQ2
Entry DOI10.2210/pdb6tq2/pdb
DescriptorBromodomain-containing protein 2, SULFATE ION, 5-[5-(4-fluorophenyl)-1~{H}-imidazol-4-yl]-1-methyl-pyridin-2-one, ... (5 entities in total)
Functional Keywordsinhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription
Biological sourceHomo sapiens (Human)
Total number of polymer chains3
Total formula weight55373.92
Authors
Chung, C. (deposition date: 2019-12-15, release date: 2020-02-19)
Primary citationWellaway, C.R.,Amans, D.,Bamborough, P.,Barnett, H.,Bit, R.A.,Brown, J.A.,Carlson, N.R.,Chung, C.W.,Cooper, A.W.J.,Craggs, P.D.,Davis, R.P.,Dean, T.W.,Evans, J.P.,Gordon, L.,Harada, I.L.,Hirst, D.J.,Humphreys, P.G.,Jones, K.L.,Lewis, A.J.,Lindon, M.J.,Lugo, D.,Mahmood, M.,McCleary, S.,Medeiros, P.,Mitchell, D.J.,O'Sullivan, M.,Le Gall, A.,Patel, V.K.,Patten, C.,Poole, D.L.,Shah, R.R.,Smith, J.E.,Stafford, K.A.J.,Thomas, P.J.,Vimal, M.,Wall, I.D.,Watson, R.J.,Wellaway, N.,Yao, G.,Prinjha, R.K.
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
J.Med.Chem., 63:714-746, 2020
Cited by
PubMed: 31904959
DOI: 10.1021/acs.jmedchem.9b01670
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.26 Å)
Structure validation

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