Table 3.

Table of selective mouse MC4R antagonists. Selectivity was defined to be greater than 100-fold more potent between at least two receptors (two pA₂ units). Ligands are grouped by possessing or not possessing agonist or antagonist activity at the mMC3R at concentrations up to 10 μM (pA₂ < 5). In some publications, numerous ligands were reported with the same selectivity profiles. In these instances, only the most potent ligands were chosen.

First Author	Year	Ref	Compound ID	Receptor Activity
				mMC1R EC50 (nM)	mMC3R pA2	mMC4R pA2	mMC5R EC50 (nM)
Ericson, Mark D	2015	[133]	17	20000 nM	< 5	8.2	>100000
Doering, Skye R	2015	[132]	3	8300 nM	< 5	7.1	24000 nM
Ericson, Mark D	2015	[133]	10	1500 nM	< 5	7	>100000
Doering, Skye R	2015	[132]	2	21000 nM	< 5	6.3	7800 nM
Ericson, Mark D	2015	[133]	22	75% @ 100μM	6.9	9.1	>100000
Lensing, Cody J	2016	[134]	10	110 nM	6.1	8.4	70% @ 100μM
Doering, Skye R	2015	[132]	6	5500 nM	5.9	8.3	20000 nM
Doering, Skye R	2015	[132]	7	5800 nM	5.7	8.3	20000 nM
Doering, Skye R	2015	[132]	1	2000 nM	5.4	7.8	2800 nM
Ericson, Mark D	2015	[133]	19	13000 nM	5.6	7.8	>100000