Literature DB >> 26101559

Target (In)Validation: A Critical, Sometimes Unheralded, Role of Modern Medicinal Chemistry.

Ramzi F Sweis1.   

Abstract

Small molecule drug discovery commonly ventures into previously unknown and unexplored target space. For such programs, an important role of medicinal chemistry is to generate molecules that enable the most reliable conclusions from a preclinical target validation/invalidation study. Multiple facets of chemistry that provide the most rigorous results for such an experiment are highlighted.

Keywords:  Target validation; biomarkers; inactive controls; proof-of-concept; target invalidation

Year:  2015        PMID： 26101559      PMCID： PMC4468394          DOI： 10.1021/acsmedchemlett.5b00183

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


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