ml347 and pyrazolo(1-5-a)pyrimidine

ml347 has been researched along with pyrazolo(1-5-a)pyrimidine* in 1 studies

Other Studies

1 other study(ies) available for ml347 and pyrazolo(1-5-a)pyrimidine

Article	Year
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN Bioorganic & medicinal chemistry letters, 2013, Jun-01, Volume: 23, Issue:11 A structure-activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189, 2, and DMH1, 3, 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. Topics: Activin Receptors, Type I; Animals; Bone Morphogenetic Protein Receptors; Half-Life; Heterocyclic Compounds, 2-Ring; Humans; Mice; Protein Binding; Protein Isoforms; Pyrazoles; Pyrimidines; Quinolines; Rats; Structure-Activity Relationship	2013

Article

Year

Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN

Bioorganic & medicinal chemistry letters, 2013, Jun-01, Volume: 23, Issue:11

A structure-activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189, 2, and DMH1, 3, 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.

Topics: Activin Receptors, Type I; Animals; Bone Morphogenetic Protein Receptors; Half-Life; Heterocyclic Compounds, 2-Ring; Humans; Mice; Protein Binding; Protein Isoforms; Pyrazoles; Pyrimidines; Quinolines; Rats; Structure-Activity Relationship

2013