. 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 3.

Comparison of Peptidomimetics 21a-c, 23a-e with Modification of R³ and R⁴


Compound	R³	R⁴	cLogP^a	RLVs (%)^b
2			−0.50	79.4 ± 1.3%
21a	1-adamantanecarbonyl	-Me	3.65	4.7 ± 0.2
21b	Fmoc	-Me	4.85	76.9 ± 4.9
21c	acetyl	-Me	1.45	95.0 ± 3.3
23a	1-adamantanecarbonyl		4.20	5.0 ± 0.7
23b	1-adamantanecarbonyl		3.65	5.1 ± 0.5
23c	1-adamantanecarbonyl		3.41	13.1 ± 0.8
23d	1-adamantanecarbonyl		4.81	33.6 ± 1.9
23e	1-adamantanecarbonyl		5.35	43.4 ± 2.4

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.