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. Author manuscript; available in PMC: 2019 Mar 25.
Published in final edited form as: Eur J Med Chem. 2018 Feb 7;148:210–220. doi: 10.1016/j.ejmech.2018.01.098

Table 3.

Inhibition of LSD1/CoREST by 11 and truncated cyclicpeptides 21–23.

Cmpd Sequence # of
residues		 %
inhibition
of LSD1 at
500 nM
11 H-AR Inline graphicM-c[K5TARKE10]TGG-KAPRKQLA-OH 21 99.20 ± 0.8 IC50 136 nM
21 H-AR Inline graphicM c[K5TARK9E10]TGG-K14APRK-NH2 18 98.05 + 0.57
22 H-AR Inline graphicM c[K5TARK9E10]TGG-K14A-NH2 15 73.43 ± 3.75
23 H-AR Inline graphicM c[K5TARK9E10]TG-NH2 12 67.31 ± 5.81
24 H-AR Inline graphicM c[K5TARK9E10] -NH2 10 59.78 ± 5.71

Percent inhibition values reported are the average of 3 determinations obtained during a single experiment + S.E.M.. The Ala residues represented in red are those replacing the original residue; positions 1, 7, and 15 are Ala residues already present in 11. SEM values and 95% confidence intervals for these % inhibition values are reported in Table S10 in the supporting information.