In vitro activity: ML347 also shows potency in BMP-responsive C2C12BRA cells with IC50 of 15 nM, and designated an MLPCN probe. ML347 displays high plasma protein binding in human, rat and mouse plasma.

Kinase Assay: ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows>300-fold selectivity for ALK2 vs. ALK3. IC50 value: Target: ALK1/ALK2 ML347 has IC50’s of 46 and 32 nM, respectively, against ALK1 and ALK2; however, the IC50 against ALK3 is 10,800 nM,>300-fold selective over ALK3. ML347 is completely inactive against all the other kinases tested (with weak activity against ALK6, 9830 nM and KDR (VEGFR2)19,700 nM). ML347 is potent in the BMP4 cell assay (152 nM).

Cell Assay: ML347 also shows effective inhibition with IC50 value of 152nM in the BMP4 cell based assay using C2C12BRA cells.