2. Academic Validation
  3. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

  • ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. doi: 10.1021/acsmedchemlett.5b00380.
Kenneth W Duncan 1,  Nathalie Rioux 1,  P Ann Boriack-Sjodin 1,  Michael J Munchhof 1,  Lawrence A Reiter 1,  Christina R Majer 1,  Lei Jin 1,  L Danielle Johnston 1,  Elayne Chan-Penebre 1,  Kristy G Kuplast 1,  Margaret Porter Scott 1,  Roy M Pollock 1,  Nigel J Waters 1,  Jesse J Smith 1,  Mikel P Moyer 1,  Robert A Copeland 1,  Richard Chesworth 1
Affiliations

Affiliation

  • 1 Epizyme, Inc. , 400 Technology Square, Cambridge, Massachusetts 02139, United States.
PMID: 26985292 DOI: 10.1021/acsmedchemlett.5b00380
Abstract

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).

Keywords

Methyltransferase; PRMT5; property based optimization; structure guided design.

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