TABLE 7

Pharmacology of human MAS-related G protein–coupled receptors X2

Potency of the ligand is given as the EC₅₀ value. The lowest concentration (LC) used to elicit a significant effect when measuring the respective readout is given. Data were generated after recombinant MRGPRX2 expression, despite when endogenous expression is indicated by “(e)”.

Ligand	EC₅₀	LC	Readout	System	Reference
	nM
Cortistatin-14	25		calcium	HEK293-Gα₁₅	Robas et al., 2003
	50		calcium	CHO	Kamohara et al., 2005
	65		cAMP inhibition	CHO	Kamohara et al., 2005
	30		GTPγS	CHO	Kamohara et al., 2005
	2000		calcium	HEK293	Burstein et al., 2006
	610		calcium	CHO-Gα₁₆	Shemesh et al., 2008
	500		calcium	HEK293	Malik et al., 2009
PAMP1-12	60		calcium	CHO	Kamohara et al., 2005
	40		cAMP inhibition	CHO	Kamohara et al., 2005
	20		GTPγS	CHO	Kamohara et al., 2005
Substance P	8000		calcium	HEK293	Tatemoto et al., 2006
Benzimidazole derivates	400		calcium	HEK293	Malik et al., 2009
SLIGKVamide	N.D.		calcium	CHO	Liu et al., 2011
PMX-53		100	calcium	LAD2 (e), RBL-2H3, human mast cells (e)	Subramanian et al., 2011b
PMX-53		10	degranulation	LAD2 (e), RBL-2H3, human mast cells (e)	Subramanian et al., 2011b
E7		1000	calcium	HMC-1 (e), LAD2 (e), human mast cells (e)	Kashem et al., 2011
E7		10	degranulation	HMC-1 (e), LAD2 (e), human mast cells (e)	Kashem et al., 2011
Substance P		100	degranulation	human mast cells (e)	Tatemoto et al., 2006
LL-37		100	calcium	LAD2 (e), HMC-1, RBL-2H3, human mast cells (e)	Subramanian et al., 2011a
LL-37		1000	degranulation	LAD2 (e), HMC-1, RBL-2H3, human mast cells (e)	Subramanian et al., 2011a
β-Defensins		100	calcium	LAD2 (e), RBL-2H3, HEK293, murine mast cells, human mast cells (e)	Subramanian et al., 2013
β-Defensins		100	degranulation		Subramanian et al., 2013

GTPγS, guanosine 5′-3-O-(thio)triphosphate; N.D., not determined.