TABLE 6

Antagonists for the human formyl peptide receptors Antagonists for the FPRs are listed in the order of their approximate potency, except that antagonists of same types are listed together.

Ligand Assay Potency Selectivity References
Chemotaxis inhibitory protein of S. aureus (CHIPS) Binding pKd = 7.46 FPR1 Haas et al. (2004)
FPRL1-inhibitor protein (FLIPr) Binding, Ca2+ flux N.D. FPR2/ALX ≫ FPR1 Prat et al. (2006)
Trp-Arg-Trp-Trp-Trp-Trp (WRW4) Ca2+ flux pIC50 = 6.64 FPR2/ALX ≫ FPR1 ≈ FPR3 Bae et al. (2004)
CsH Binding pKi = 7.00 FPR1 Wenzel-Seifert et al. (1991)
CsA Enzyme release pKi = 6.22 FPR1 Yan et al. (2006)
i-Boc-Met-Leu-Phe O2 generation pIC50 = 6.60 FPR1 Derian et al. (1996)
t-Boc-Met-Leu-Phe Enzyme release pIC50 = 6.19 FPR1 Freer et al. (1980)
t-Boc-Phe-Leu-Phe-Leu-Phe Enzyme release pIC50 = 6.59 FPR1 ≫ FPR2/ALX Freer et al. (1980)
Quin-C7 Binding pKi = 5.19 FPR2/ALX Zhou et al. (2007)
CDCA Binding pKi = 4.76–4.52 FPR1 > FPR2/ALX Chen et al. (2000)
DCA Binding pKi = 4.00 FPR1 Chen et al. (2002)
Spinorphin O2 generation pIC50 = 4.30 FPR1 Yamamoto et al. (1997); Liang et al. (2000)
  • t-Boc, N-tert-butoxycarbonyl group; i-Boc, -butoxycarbonyl group; pIC50, negative logarithm of the IC50; pKi, negative logarithm of Ki; N.D., binding affinity or potency was not determined