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Title: Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors

Journal Article · · Bioorganic and Medicinal Chemistry Letters

The initial structure activity relationships around an isoindoline uHTS hit will be described. Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. These efforts allowed for the identification of a compound with properties suitable for use as an in vitro tool compound for validation studies on MARK as a viable target for Alzheimer’s disease.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
INDUSTRY
OSTI ID:
1404963
Journal Information:
Bioorganic and Medicinal Chemistry Letters, Vol. 27, Issue 1; ISSN 0960-894X
Publisher:
Elsevier
Country of Publication:
United States
Language:
ENGLISH