Figure 5.

Analysis of KDM1A target engagement and proxy markers. A, IC₅₀ determination of KDM1A target engagement by ORY-1001 in MV(4;11) cells treated for 96 h with different doses of ORY-1001 (representative luminescent immunoassay of N = 3, n = 3, mean ± S.D.). B, EC₅₀ determination of H3K4me2 accumulation induced in MV(4;11) cells by 96 h of treatment with ORY-1001 (AlphaLISA; N = 3, n = 2, mean ± S.E. (error bars)). C, EC₅₀ determination of MV(4;11) viability (Alamar Blue assay; representative experiment of N = 5, n = 3, mean ± S.D. (error bars)). D, EC₅₀ determination of LY96 gene expression changes induced in MV(4;11) cells by 96 h of treatment with ORY-1001 (qRT-PCR; N = 3, n = 3, mean ± S.E. (error bars)). Data are normalized to the GAPDH control, and -fold changes were calculated relative to the vehicle control sample.