. 2017 Feb 14;8(3):338–343. doi: 10.1021/acsmedchemlett.6b00519

Table 1. Biochemical, Biophysical, and Cellular Characterization of Lead Compound 7.

	7	EPZ-5676
IC₅₀ (Dot1L SPA)^a	<0.1	<0.1
K_i (Dot1L SPA)^a	0.002	0.012
τ (Dot1L SPR)⁺	>5	>5
IC₅₀ (HeLa, H3K79me2 ELISA)^a	3	7
IC₅₀ (Molm-13, HoxA9 RGA)^a	17	52
IC₅₀ (MV4-11, prolif.)^a	5	15

[nM], ⁺[h], all data are the results of at least two assay runs with the mean value reported. The coefficient of variation was less than 60% in all cases. Biochemical IC₅₀ values were determined at K_M for SAM. K_i values were determined by applying the Morrison tight binding model (Supporting Information).