Abstract
A four-step process of high-quality modeling of existing data, deconstruction, identification of replacement cores, and an innovative synthetic regrowth strategy led to the rapid discovery of a novel oral series of PI3Kδ inhibitors with promising selectivity and excellent in vivo characteristics.
MeSH terms
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Administration, Inhalation
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Animals
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Biological Availability
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Class Ia Phosphatidylinositol 3-Kinase / metabolism
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Dose-Response Relationship, Drug
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Male
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Models, Molecular
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Molecular Structure
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Phosphoinositide-3 Kinase Inhibitors*
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Protein Kinase Inhibitors / administration & dosage
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Respiratory Tract Diseases / drug therapy*
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Respiratory Tract Diseases / metabolism
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Structure-Activity Relationship
Substances
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Phosphoinositide-3 Kinase Inhibitors
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Protein Kinase Inhibitors
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Class Ia Phosphatidylinositol 3-Kinase