Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
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DOI: 10.1021/acs.jmedchem.2c00552
Abstract: PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification. To… read more here.
Keywords: pkmyt1 inhibitor; pkmyt1; discovery orally; orally bioavailable ... See more keywords
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01099
Abstract: Kinase fusions involving tropomyosin receptor kinases (TRKs) have been proven to act as strong oncogenic drivers and are therefore recognized as attractive therapeutic targets. We screened an in-house kinase-focused library and identified a promising hit… read more here.
Keywords: selective potent; orally bioavailable; bioavailable selective; trk inhibitor ... See more keywords