. Author manuscript; available in PMC: 2017 Nov 9.

Published in final edited form as: J Med Chem. 2016 Mar 29;59(7):3112–3128. doi: 10.1021/acs.jmedchem.5b01894

Table 2. Summary of functional experiments for based compounds evaluated at the mouse melanocortin receptors.

	mMC1R		mMC3R		mMC4R		mMC5R		Selectivity
Compound	Agonist EC₅₀ (nM)		Agonist EC₅₀ (nM)		Agonist EC₅₀ (nM)		Agonist EC₅₀ (nM)		Ratios
	Mean±SEM	Fold Diff.	Mean±SEM	Fold Diff.	Mean±SEM	Fold Diff.	Mean±SEM	Fold Diff.	1R: 3R:4R:5R
NDP-MSH	0.03±0.01^*		0.24±0.01^*		0.46±0.04^*		0.31±0.03^*		1:9:18:12
α-MSH	0.15±0.05		0.76±0.05		4.0±0.9		0.59±0.03		1:5:28:4
Ɣ-MSH	1090±300		34.6±4.0		869±66		35.1±18.7		31:1:25:1
1	14.1±2.6^*	1	55.5±12.2^*	1	13.7±1.9^*	1	9.8±2.7^*	1	1:4:1:1
2	26.2±9.9	0.5	47.4±12.7	1	5.7±2.9	2	2.1±0.3	5	13:23:3:1
3	24.9±5.9^*	0.6	30.9±7.5^*	2	18.5±2.9^*	0.7	3.9±1.3^*	2	6:8:5:1
4	5.7±.7	2	107±66	0.5	74.1±14.1	0.2	52.4±10.3	0.2	1:19:13:9
5	16.4±4.7^*	0.9	27.2±5.2^*	2	14.5±2.7^*	0.9	4.9±1.2^*	2	3:6:3:1
6	4.4±0.6^*	3	20.2±4.0^*	3	9.2±1.0^*	1	3.8±0.9^*	2	1:5:2:1
7	6.4±1.5^*	2	10.1±2.5^*	5	3.6±0.5^*	4	3.1±0.6^*	3	1:3:1:1
8	12.6±3.8	1	22.7±3.7	2	7.3±2.1	2	4.0±0.2	2	3:6:2:1

AlphaScreen® assays were performed to determine relative potency of compounds to induce cAMP signaling. The reported errors are the standard error of the mean (SEM) determined from at least three independent experiments. Changes less than 3-fold were considered to be within the inherent experimental assay error.

denotes six or more independent experiments.