. Author manuscript; available in PMC: 2014 Nov 1.

Published in final edited form as: Bioorg Med Chem Lett. 2013 Sep 7;23(21):5814–5820. doi: 10.1016/j.bmcl.2013.08.111

Table 1.

Summary of IC₅₀ values determined by Lgr5 and Axin2 gene expression

graphic file with name nihms544246u1.jpg

No.	Core	R	R¹	Lgr5 IC₅₀ (μM) (Mean +/− SEM)	Axin2 IC₅₀ (μM) (Mean +/− SEM)
1	calphostin C			0.39 +/− 0.19	0.55 +/− 0.18
2	XAV939			2.9	0.64
3	xanthothricin			0.29 +/− 0.02	0.33 +/− 0.03
8a	A	Me	OMe	1.53 +/− 0.37	2.67 +/− 0.62
8b	A	Me	OCH₂CH₂NEt₂	NI up to 0.7 μM	NI up to 0.7 μM
8c	A	Me	Cl	1.53 +/− 0.42	1.77 +/− 0.28
10a	A	CH₂CH₂OH	OMe	NI up to 1.2 μM	NI up to 1.2 μM
10b	A	Ph	OMe	2.1 +/− 0.32	2.67 +/− 0.33
11c	A	Ph	OCH₂CH₂NEt₂	0.26 +/− 0.11	0.30 +/− 0.11
20a	B	Me	OCH₂CH₂NEt₂	NI up to 69 μM	NI up to 69 μM
20b	B	Ph	OCH₂CH₂NEt₂	164.7	PI up to 179 μM

NI – No inhibition

PI – Partial inhibition