TABLE 2.

Trp-based derivatives that induced Ca²⁺ mobilization in human neutrophils and FPR-transfected HL-60 cells

The EC₅₀ values are presented as the mean ± S.D. of three independent experiments, in which median effective concentration values (EC₅₀) were determined by nonlinear regression analysis of the dose-response curves (five to six points) generated using GraphPad Prism 5 with 95% confidence interval (P < 0.05). Efficacy is expressed as percentage of the response induced by 5 nM fMLF (FPR1) or 5 nM WKYMVm (FPR2 and FPR3).

Compound	R1	R2	Enantiomer	Ca2+ Mobilization, EC50, and Efficacy
				Neutrophils	FPR1	FPR2	FPR3
				μM (%)
AG-10/1	H		R/S	3.8 ± 0.5 (120)	2.7 ± 0.4 (100)	0.3 ± 0.07 (115)	13.5 ± 3.4 (60)
AG-10/2	Br		S	1.9 ± 0.5 (125)	0.5 ± 0.1 (120)	0.13 ± 0.03 (120)	7.6 ± 1.9 (85)
AG-10/3	Br		S	2.7 ± 0.6 (135)	2.2 ± 0.6 (120)	0.3 ± 0.06 (110)	2.4 ± 0.5 (80)

N.A., nonactive compound (cell activation was <30% of control level over a concentration range of 0–40 μM).

*Location of the chiral center.