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Development of a Potent and ALK2 Selective Bone Morphogenetic Protein Receptor (BMP) Inhibitor

Development of a Potent and ALK2 Selective Bone Morphogenetic Protein Receptor (BMP) Inhibitor

Darren W. Engers, Audrey Y. Frist, Craig W. Lindsley, Charles H. Hong, Corey R. Hopkins

PMID: 25506972

Abstract:

A fast-track chemistry effort was initiated to evaluate the structure-activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known bone morphogenetic protein (BMP) inhibitors. This medicinal chemistry effort led to the identification of a potent and selective compound for ALK2 versus ALK3. The potency contributions of several 3-position substituents were evaluated with subtle structural changes leading to significant changes in potency. From these studies, a novel 5-quinoline molecule was identified and designated an MLPCN probe molecule, ML347, which shows >300-fold selectivity for ALK2 and presents the community with a selective molecular probe for further biological evaluation.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1062368493	ML347		1062368-49-3	Price

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