Table 1. Inhibitory Activities of Compounds 5–11 against hPRMT1.

^aAlphaLISA was used for both fixed dose and IC₅₀ determinations against human recombinant PRMT1 (0.9 nM, final concentration). Histone H4 (1–21) peptide, biotinylated (100 nM, final concentration), and SAM (2 μM, final concentration) were used as substrate and cofactor, respectively.

^bCompounds were tested at a 100 μM fixed concentration.

^cEnzyme residual activity percentage calculated with respect to DMSO.

^dCompounds were tested in 10-concentration IC₅₀ mode with threefold serial dilutions starting at 100 μM. Data were analyzed with GraphPad Prism software (version 6.0) for IC₅₀ curve fitting.

^eLigand efficiency (LE) calculated from IC₅₀ as a surrogate for K_D.

^fND, not determined.