1616059-87-0Relevant articles and documents
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666
Duncan, Kenneth W.,Rioux, Nathalie,Boriack-Sjodin, P. Ann,Munchhof, Michael J.,Reiter, Lawrence A.,Majer, Christina R.,Jin, Lei,Johnston, L. Danielle,Chan-Penebre, Elayne,Kuplast, Kristy G.,Porter Scott, Margaret,Pollock, Roy M.,Waters, Nigel J.,Smith, Jesse J.,Moyer, Mikel P.,Copeland, Robert A.,Chesworth, Richard
, p. 162 - 166 (2016/03/01)
The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool compound EPZ015666 (GSK3235025) to probe the underlying pharmacology of this key enzyme. Herein, we report the design and optimization strategies employed on an initial hit compound with poor in vitro clearance to yield in vivo tool compound EPZ015666 and an additional potent in vitro tool molecule EPZ015866 (GSK3203591).
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 00353, (2014/07/08)
Described herein are compounds of formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical com-positions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
