. 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 2.

Comparison of Peptidomimetics 17 and 19a-k with Modifications at R²


Compound	R²	cLogP^a	RLVs (%)^b
2		−0.50	79.4 ± 1.3%
17	-OMe	3.23	39.8 ± 3.3
19a		2.92	72.0 ± 4.4
19b		3.93	92.3 ± 3.6
19c		2.81	103.2 ± 3.6
19d		4.38	133.8 ± 2.5
19e		3.69	14.0 ± 1.2
19f		2.27	111.9 ± 1.0
19g		4.51	117.2 ± 3.0
19h		5.15	81.5 ± 3.2
19i		2.84	54.2 ± 1.8
19j		2.17	118.1 ± 2.3
19k	-Oallyl	3.80	11.9 ± 0.7

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.