Table 1. PAR2 Agonist Activities^a.

	Gq activation		β-arrestin-2 recruitment
	EC50 [μM]	Emax [%]b	EC50 [μM]	Emax [%]b
4a	3.1 ± 1.1	70 ± 7	n.c.d	6 ± 3e
4b	0.59 ± 0.10	93 ± 2	6.0 ± 0.3	65 ± 6
4c	1.0 ± 0.1	95 ± 1	n.c.d	55 ± 7e
4d	11 ± 1	108 ± 4	n.c.d	8 ± 1
4e	2.2 ± 0.3	105 ± 8	n.c.d	53 ± 10e
4f	3.3 ± 0.4	93 ± 1	n.c.d	42 ± 4e
4g	1.3 ± 0.2	97 ± 2	n.c.d	73 ± 6e
4h	2.9 ± 0.4	92 ± 3	n.c.d	41 ± 5
5a	0.64 ± 0.19	105 ± 2	8.9 ± 0.4	95 ± 3
5b	0.96 ± 0.05	104 ± 4	18 ± 2	93 ± 4
6	n.a.c	<5	n.a.c	<5
7	1.9 ± 0.1	93 ± 1	n.c.d	32 ± 4e
8a	n.c.d	85 ± 2e	n.a.c	<5
8b	n.c.d	44 ± 2e	n.a.c	<5
9	n.c.d	9 ± 1e	n.a.c	<5
10a	1.8 ± 0.3	97 ± 3	n.c.d	60 ± 2e
10b	0.64 ± 0.08	100 ± 1	7.4 ± 0.3	87 ± 6
11	2.4 ± 0.2	98 ± 5	n.c.d	93 ± 5e
12a	4.2 ± 0.5	97 ± 4	n.c.d	32 ± 4e
12b	4.9 ± 0.8	98 ± 4	n.c.d	33 ± 5e
13	n.c.d	12 ± 5e	n.a.c	<5
1	0.15 ± 0.03	100	0.43 ± 0.05	100
2	0.17 ± 0.03	110 ± 4	2.0 ± 0.2	94 ± 5

^aData are reported as mean ± SEM for at least three independent experiments performed in duplicate.

^bMaximum efficacy determined relative to reference 1 (2f-LIGRLO-NH₂).

^cn.a. indicates that no activity was observed.

^dn.c. indicates that the dose–response curve did not converge to a plateau and an exact EC₅₀ was not calculated.

^eThe dose–response curve did not converge to a plateau, and the reported value is the efficacy at a ligand concentration of 30 μM.