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Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties

Klemens Hoegenauer, Nicolas Soldermann, Christina Hebach, Gregory J. Hollingworth, Ian Lewis, Anette von Matt, Alexander B. Smith, Romain M. Wolf, Rainer Wilcken, Dorothea Haasen,

Bioorganic & Medicinal Chemistry Letters · 2016 · 20 citations · 24 references

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24

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

Frank Lovering, Jack Bikker, Christine Humblet · Journal of Medicinal Chemistry · 2009 · 4.4K citations

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Escape from Flatland 2: complexity and promiscuity

Frank Lovering · MedChemComm · 2012 · 1.4K citations

, , +12

Polar Molecular Surface as a Dominating Determinant for Oral Absorption and Brain Penetration of Drugs

J. Kelder, Peter D. J. Grootenhuis, Denis M. Bayada et al. · Pharmaceutical Research · 1999 · 799 citations

, , +13

Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis

Montserrat Camps, Thomas Rückle, Hong Ji et al. · Nature Medicine · 2005 · 751 citations

, , +15

Dominant-activating germline mutations in the gene encoding the PI(3)K catalytic subunit p110δ result in T cell senescence and human immunodeficiency

C. Lucas, Hye Sun Kuehn, Fang Zhao et al. · Nature Immunology · 2013 · 664 citations

, , +15