. Author manuscript; available in PMC: 2020 Jul 11.

Published in final edited form as: J Med Chem. 2019 Jun 27;62(13):6262–6275. doi: 10.1021/acs.jmedchem.9b00566

Table 3.

IC₅₀ Values for PeIA and Analogs with Negatively Charged Amino Acid Substitutions of Asn^11a

	α3β2 nAChR			α6/α3β2β3 nAChR
peptide	IC₅₀ (nM)	n	log change in IC₅₀	IC₅₀ (nM)	n	log change in IC₅₀	selectivity ratio
PeIA	19.4 (15.3–24.6)	5		19.8 (17.9–21.8)	4		1
[Asp¹¹]PeIA	54.0 (45.7–64.5)	6	0.4	362 (215–611)	6	1.3	7
[Glu¹¹]PeIA	31.1 (27.0–36.0)	4	0.2	114 (92.7–140)¹³	4	0.8	4
[Aadⁿ]PeIA	123 (96.9–157)	6	0.8	>10 000	5	>2.7	81
[Api¹¹]PeIA	18.1 (14.8–22.2)	4	–0.1	5432 (2809–10 500)	4	2.4	300
[Asu¹¹]PeIA	44.4 (40.2–49.0)	4	0.4	2605 (1628–4168)	4	2.1	59

Values in parentheses indicate the 95% CI of the IC₅₀ values. Changes in potency were calculated as the log(analog IC₅₀)/(PeIA IC₅₀), negative values indicate increased potency and positive values indicate decreased potency. Selectivity was calculated as the IC₅₀ ratio of (α6/α3β2β3)/(α3β2).