Table 10.

Intracellular signaling cascades triggered by ligands from nonpeptide library.

Ligand	Origin	Selectivity	Cells	Effects	Ref.	Potency
Quin-C1	Combinatorial library	FPR2	Neutrophils; FPR2-expressing cells	chemotaxis; β-glucuronidase secretion	[142]	pEC50 = 5.72
			FPR2/RBL	Ca2+ mobilization; ERKs activation	[142]
			Mouse model	anti-inflammatory; reduction of the expression of TNF-α, IL-1β, keratinocyte-derived chemokine, TGF-β1 and CXCL10	[143]
Pyrazolone 24/43	Combinatorial library	FPR2	FPR2-transfected cells	anti-inflammatory; Ca2+ mobilization	[144]	pIC50 = 7.36
Aryl carboxylic acid hydrazide derivatives	Chemolibrary of drug-like molecules	FPR2	Monocytes; Macrophages; Phagocytes	TNFα production; Ca2+ mobilization; reactive oxygen species production; chemotaxis	[145]	EC50 = 2 μM
Pyridazin-derivatives	Ligand-based drug design approach	FPR1/FPR2	Neutrophils	Ca2+ mobilization; chemotaxis	[146]	EC50 = 13.1 μM
AG-26, AG-09/4-AG09/8	Chemolibrary of drug-like molecules	FPR2	FPR2-transfected RBL-2H3	Ca2+ mobilization	[84]	EC50 = 0.5 μM, 0.3–12.6 μM
PD168368; PD176252; A-716223	Screening of known GPCR ligands	FPR1/FPR2	FPRs-transfected HL-60; Neutrophils	Ca2+ mobilization; reactive oxygen species production	[147]	EC50 = 0.5 μM, 0.9 μM, 18.3 μM

pEC₅₀, negative logarithm of the EC₅₀; pIC₅₀, negative logarithm of the IC₅₀.