MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation

[Display omitted] Attempts to optimize pharmacokinetic properties in a promising series of pyrrolopyrimidinone MARK inhibitors for the treatment of Alzheimer’s disease are described. A focus on physical properties and ligand efficiency while prosecuting this series afforded key tool compounds that r...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-01, Vol.27 (1), p.109-113
Hauptverfasser:	Haidle, Andrew M., Childers, Kaleen K., Zabierek, Anna A., Katz, Jason D., Jewell, James P., Hou, Yongquan, Altman, Michael D., Szewczak, Alexander, Chen, Dapeng, Harsch, Andreas, Hayashi, Mansuo, Warren, Lee, Hutton, Michael, Nuthall, Hugh, Stanton, Matt G., Davies, Ian W., Munoz, Ben, Northrup, Alan
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer Disease - drug therapy Alzheimer Disease - metabolism Animals Disposition study Dose-Response Relationship, Drug Humans In vitro–in vivo correlation Isoenzymes - antagonists & inhibitors Isoenzymes - metabolism Kinase MARK Molecular Structure Optimization Pharmacokinetics Physical properties Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - metabolism Pyrimidinones - chemistry Pyrimidinones - metabolism Pyrimidinones - pharmacology Pyrroles - chemistry Pyrroles - metabolism Pyrroles - pharmacology Rats Structure-Activity Relationship
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