Table 2.

Summary of small molecule US28 modulators. Their groups, names of compounds, types, mechanisms, EC₅₀ values, chemical structures, and references were also included

Group	Compound	Type	Mechanism	EC50 (μm)	Chemical structure	Reference
VUF2274	5-(4-(4-chlorophenyl)-4-hydroxy-piperidin-1-yl)-2,2-diphenylpentanenitrile	Inverse agonist	Constitutive PLCb activation CCL5 binding	4.5		Tschammer, 2014
Methiothepin		Antagonist	CCL5 binding	0.4		Fraile-Ramos et al., 2001
Hydroisoquinoline	3-(2-hydroxyethyl)-3-methyl-2-phenyl03,4-dihydroisoquinolin-1(2H)-one	Inverse agonist	Constitutive PLCb activation	1.5		Kralj et al., 2011
	N-(2-aminoethyl)-N-((3-methyl-1-oxo-1,2,3,4-tetrahydroisoquinolin-3-yl)methyl)decanamide	Inverse agonist	Constitutive PLCb activation	1.5		Kralj et al., 2011
	3-(2-hydroxyethyl)-3-methyl-2-phenyl-3,4-dihydroisoquinolin-1(2H)-one	Inverse agonist	Constitutive PLCb activation	1.0		Kralj et al., 2011
	(3-methyl-1-oxo-2-(2-phenylacetyl)-1,2,3,4-tetrahydroisoquinolin-3-yl)methyl 2-phenylacetate	Inverse agonist	Constitutive PLCb activation	3.4		Vischer et al., 2010
Biphenyl amide	Decanoic acid (4′-chloro-6-methoxybiphen-3-ylmethyl)-(2-dimethylaminoethyl) amide	Inverse agonist	Constitutive PLCb activation	2.4		Kralj et al., 2014
Flavonoid	5-(benzyloxy)-2-(5-bromo-2-methoxyphenyl)-4H-chromen-4-one	Inverse agonist	Constitutive PLCb activation	3.5		Kralj et al., 2013
Other	(4-(4-chlorophenyl)-1-(4,4-diphenylbutyl)piperidin-4-yl)	Antagonist	CCL5 binding	3.6		Hulshof et al., 2006