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. 2016 Oct 14;59(21):9928–9941. doi: 10.1021/acs.jmedchem.6b01315

Table 1. Piperidine Structure–Activity Relationships.

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a

Biochemical data generated via scintillation proximity assay (SPA) with PRC2, H3K27me3 activator peptide and biotinylated oligonucleosomes and 3[H]-SAM. IC50 values reported as an average ≥2 determinations.

b

The mechanism of action cellular assay measured global H3K27me3 levels in HeLa cells; see Supporting Information for further details.

c

pKa values generated via ChemDraw version 15.0

d

IC50 value from a single determination.