Table 1. PAR2-Targeted Peptides (1, 2, and 6–12) 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 |
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).