Skip to main content
. 2019 Jun 6;10(7):1045–1050. doi: 10.1021/acsmedchemlett.9b00094

Table 1. PAR2-Targeted Peptides (1, 2, and 612) with Their EC50 and LogD Valuesa.

# compound EC50 (nM) pEC50 ± SEM LogD ± SEM
1 SLIGRL-NH2 7144 5.15 ± 0.03 –1.02 ± 0.02
2 2f-LIGRLO-NH2 210 6.68 ± 0.04 –1.06 ± 0.01
6 Isox-Cha-Chg-NH2 2555 5.59 ± 0.10 2.00 ± 0.02
7 Isox-Cha-Chg-AR-NH2 14 7.86 ± 0.06 –0.15 ± 0.01
8 Isox-Cha-Chg-AR-NH(CH2)6NH2 16 7.79 ± 0.04 –0.40 ± 0.01
9 Isox-Cha-Chg-ARLK-NH2 23 7.65 ± 0.07 –0.72 ± 0.02
10 Isox-Cha-Chg-ARAK-NH2 15 7.82 ± 0.07 –1.58 ± 0.04
11 Isox-Cha-Chg-ARK-NH2 10 8.00 ± 0.09 –0.86 ± 0.02
12 Isox-Cha-Chg-ARK(COCH3)-NH2 16 7.78 ± 0.05 –0.24 ± 0.02
a

EC50 values determined through a dose–response curve from a β-arrestin 2 recruitment assay in HEK293T cells transiently transfected with PAR2-eYFP/Arr2-rluc BRET pair (n ≥ 3). LogD values were determined at a physiological pH of 7.4 (n = 3).