. Author manuscript; available in PMC: 2018 Oct 1.

Published in final edited form as: Biochim Biophys Acta. 2017 Mar 29;1863(10 Pt A):2414–2435. doi: 10.1016/j.bbadis.2017.03.020

Table 1.

Table of selective melanocortin agonists for the human MCRs. Selectivity was defined to be at least 100-fold more potent between at least two receptor subtypes. Ligands are grouped by receptor selectivity. In some publications, numerous ligands were reported with the same selectivity profiles. In these instances, only the most potent ligands were chosen.

Selective For:	First Author	Year	Ref	Compound ID	Compound EC₅₀ (nM)

					hMC1R	hMC3R	hMC4R	hMC5R
hMC1R	Bednarek, Maria A	2007	[119]	11	*1.4 (59%)*	0.54 (43%)	4% @ 2.5μM	0.11
	Cai, Minying	2015	[121]	1	15	>10000	>10000	7
	Bednarek, Maria A	2007	[119]	5	*0.23 (67%)*	3% @ 2.5μM	0% @ 2.5μM	0.088
	Bednarek, Maria A	2007	[120]	2	90	0% @ 10μM	0% @ 10μM	50
	Conde-Frieboes, K	2011	[122]	6a	12	>10000	700	>10000
	Conde-Frieboes, K	2011	[122]	7	16	>10000	470	>10000
	Cai, Minying	2015	[121]	15	*3.7*	>10000	>10000	>10000
	Cai, Minying	2015	[121]	8	*2.1*	>10000	>10000	450
	Bednarek, Maria A	2007	[123]	2	*2.4*	34% @ 1μM	22% @ 2.5μM	26% @ 1.5μM

hMC3R	Bednarek, Maria A	2007	[119]	11	1.4 (59%)	*0.54 (43%)*	4% @ 2.5μM	0.11
hMC3R	Carotenuto, Alfonso	2015	[127]	2	940	*1.9*	>1000	10

hMC4R	Hong, Qingmei	2010	[128]	21A	1200	90	*5.4*	490
	Hong, Qingmei	2010	[128]	23A	520	79	*6.4*	1000
	Hong, Qingmei	2010	[128]	20B	540	1800	13	>5000
	Hong, Qingmei	2010	[128]	25B	>5000	2500	19	>5000
	Cai, Minying	2015	[121]	17	>10000	>10000	*5 (67%)*	>10000

hMC5R	Bednarek, Maria A	2007	[119]	11	1.4 (59%)	0.54 (43%)	4% @ 2.5μM	*0.11*
	Cai, Minying	2015	[121]	1	15	>10000	>10000	7
	Bednarek, Maria A	2007	[119]	5	0.23 (67%)	3% @ 2.5μM	0% @ 2.5μM	*0.088*
	Bednarek, Maria A	2007	[120]	23	3.8 (46%)	8% @ 5μM	3% @ 5μm	*0.15*
	Bednarek, Maria A	2007	[119]	7	20% @ 5μM	54% @ 5μM	36% @ 5μM	*0.41*