. Author manuscript; available in PMC: 2021 Oct 22.

Published in final edited form as: J Med Chem. 2020 Oct 15;63(20):11522–11547. doi: 10.1021/acs.jmedchem.0c00531

Table 1.

Comparison of Tetra-peptidomimetics 11, 12, 13a-g and Tripeptide Analogs 30–32


Compound	R¹ (for peptidomimetics 11, 12, 13a-g)	cLogP^a	RLVs (%)^b
2		−0.50	79.4 ± 1.3%
11	Cbz	2.55	112.3 ± 6.1
12	-H	0.50	114.1 ± 3.2
13a		2.05	105.1 ± 6.8
13b		2.89	83.5 ± 2.8
13c		2.96	68.7 ± 2.5
13d		3.88	114.5 ± 3.0
13e		2.32	103.9 ± 5.8
13f		2.19	122.6 ± 3.0
13g		1.74	86.4 ± 2.7
30		3.10	>100%
31		1.94	>100%
32		2.63	>100%

clogP: http://biosig.unimelb.edu.au/pkcsm/prediction.

Results from screening compounds (50 μM; n = 4 replicates per compound) against the FGF14:Na_v1.6 complex using the LCA in HEK293 cells are shown as relative luminescence values (RLVs), which are calculated as percent luminescence relative to the mean of per plate controls (0.5% DMSO; n = 32 replicates per plate). Values are mean ± SEM over at least three independent experiments.