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. Author manuscript; available in PMC: 2019 Dec 20.
Published in final edited form as: Cell Chem Biol. 2018 Sep 6;25(12):1443–1455.e14. doi: 10.1016/j.chembiol.2018.08.004

Figure 2: 12-membered macrolactams are inhibitors of BAF-mediated transcription.

Figure 2:

A. The EC50 was measured for the best screen hit BRD-K98645985 after 24 h compound treatment with the Bmi1-luciferase reporter cell line. Each concentration was dosed in triplicate. B. The fold change of the transcription of three BAF target genes was calculated using qRT-PCR after 18 h BRD-K98645985 treatment (30 µM) or Brg1 knockdown compared to untreated cells. C. Viability measurements in wild type ESCs were performed after 72 h of compound or DMSO treatment using CellTiter-Glo®. D. The structure activity relationship of the eight stereoisomers of BRD- K98645985 based on initial luciferase induction from the primary screen. E. The structure activity relationship of the 3618 macrolactam library members based on initial luciferase induction from the primary screen. See also Figure S2.