TABLE 6.
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.