Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET

Luke W. Koblan; Dennis L. Buckley; Christopher J. Ott; Mark E. Fitzgerald; Stuart W.J. Ember; Jin Yi Zhu; Shuai Liu; Justin M. Roberts; David Remillard; Sarah Vittori; Wei Zhang; Ernst Schonbrunn; James E. Bradner

doi:10.1002/cmdc.201600502

Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET

Luke W. Koblan
, Dennis L. Buckley
, Christopher J. Ott
, Mark E. Fitzgerald
, Stuart W.J. Ember
, Jin Yi Zhu
, Shuai Liu
, Justin M. Roberts
, David Remillard
, Sarah Vittori
, Wei Zhang
, Ernst Schonbrunn
, James E. Bradner

Chemistry

Research output: Contribution to journal › Article › peer-review

Original language	English
Pages (from-to)	2575-2581
Number of pages	7
Journal	ChemMedChem
Volume	11
Issue number	23
DOIs	https://doi.org/10.1002/cmdc.201600502
State	Published - Dec 6 2016

ASJC Scopus Subject Areas

Biochemistry
Molecular Medicine
Pharmacology
Drug Discovery
General Pharmacology, Toxicology and Pharmaceutics
Organic Chemistry

Keywords

bromodomain inhibition
drug design
epigenetics
fluorescence
in-cell target engagement assays
luminescence

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10.1002/cmdc.201600502

Cite this

Koblan, L. W., Buckley, D. L., Ott, C. J., Fitzgerald, M. E., Ember, S. W. J., Zhu, J. Y., Liu, S., Roberts, J. M., Remillard, D., Vittori, S., Zhang, W., Schonbrunn, E., & Bradner, J. E. (2016). Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET. ChemMedChem, 11(23), 2575-2581. https://doi.org/10.1002/cmdc.201600502

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title = "Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET",

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author = "Koblan, \{Luke W.\} and Buckley, \{Dennis L.\} and Ott, \{Christopher J.\} and Fitzgerald, \{Mark E.\} and Ember, \{Stuart W.J.\} and Zhu, \{Jin Yi\} and Shuai Liu and Roberts, \{Justin M.\} and David Remillard and Sarah Vittori and Wei Zhang and Ernst Schonbrunn and Bradner, \{James E.\}",

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year = "2016",

month = dec,

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doi = "10.1002/cmdc.201600502",

language = "English",

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AU - Koblan, Luke W.

AU - Buckley, Dennis L.

AU - Ott, Christopher J.

AU - Fitzgerald, Mark E.

AU - Ember, Stuart W.J.

AU - Zhu, Jin Yi

AU - Liu, Shuai

AU - Roberts, Justin M.

AU - Remillard, David

AU - Vittori, Sarah

AU - Zhang, Wei

AU - Schonbrunn, Ernst

AU - Bradner, James E.

PY - 2016/12/6

Y1 - 2016/12/6

KW - bromodomain inhibition

KW - drug design

KW - epigenetics

KW - fluorescence

KW - in-cell target engagement assays

KW - luminescence

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UR - https://www.scopus.com/pages/publications/85000386279#tab=citedBy

U2 - 10.1002/cmdc.201600502

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M3 - Article

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AN - SCOPUS:85000386279

SN - 1860-7179

VL - 11

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JO - ChemMedChem

JF - ChemMedChem

IS - 23

ER -

Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET

ASJC Scopus Subject Areas

Keywords

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