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J Med Chem. 2019 Nov 27;62(22):10402-10422. doi: 10.1021/acs.jmedchem.9b01499. Epub 2019 Nov 6.

Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of N-Methylation for PI3Kδ Activity.

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GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, School of Chemistry , University of Nottingham , Triumph Road , Nottingham NG7 2TU , U.K.
GlaxoSmithKline, Medicines Research Centre , Gunnels Wood Road , Stevenage SG1 2NY , U.K.


Phosphoinositide-3-kinase δ (PI3Kδ) is a critical regulator of cell growth and transformation and has been explored as a therapeutic target for a range of diseases. Through the exploration of the thienopyrimidine scaffold, we have identified a ligand-efficient methylation that leads to remarkable selectivity for PI3Kδ over the closely related isoforms. Interrogation through the Free-Wilson analysis highlights the innate selectivity the thienopyrimidine scaffold has for PI3Kδ and provides a predictive model for the activity against the PI3K isoforms.

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