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. Author manuscript; available in PMC: 2018 Jun 13.
Published in final edited form as: J Med Chem. 2017 Nov 13;60(22):9320–9329. doi: 10.1021/acs.jmedchem.7b01295

Table 2.

Competitive Binding Assay and cAMP Assay Results of γ-MSH Analoguesa

no. hMC1R
hMC3R
hMC4R
hMC5R
IC50, nM % BE EC50, nM % max effect IC50, nM % BE EC50, nM % max effect IC50, nM % BE EC50, nM % max effect IC50, nM % BE EC50, nM % max effect
1 0.30 ± 0.02 100 3.0 ± 0.2 70 5.0 ± 0.6 100 300 ± 6 6 6.0 ± 1 100 630 ± 70 18 3.5 ± 0.5 100 NA 6
2 82 ± 7 100 4.6 ± 0.9 100 4.1 ± 0.4 100 5.0 ± 0.4 100 5.0 ± 0.4 100 23 ± 3 90 18 ± 3 100 16 ± 1 82
3 NB 0 >1000 100 18 ± 2 33 NA 0 NB 0 NA 0 NB 0 NA 0
4 137 ± 11 100 604 ± 74 100 17 ± 1 26 NA 0 >1000 47 NA 0 NB 0 NA 0
5 24 ± 3 100 4.5 ± 0.4 100 >1000 45 >1000 50 210 ± 5 58 71 ± 8 54 NB 0 NA 0
6 16 ± 2 29 NA 0 117 ± 24 32 NA 0 NB 0 NA 0 0.42 ± 0.07 32 NA 0
7 1.1 ± 0.1 32 >1000 100 >1000 47 >1000 100 6.7 ± 0.9 36 200 ± 25 100 NB 0 NA 0
8 >1000 52 40 ± 6 100 118 ± 14 73 521 ± 72 100 360 ± 42 62 128 ± 13 78 36 ± 1 47 >1000 100
9 23 ± 2 100 31 ± 6 100 56 ± 3 69 >1000 100 20 ± 1 86 444 ± 69 100 254 ± 41 38 NA 0
10 42 ± 7 100 8 ± 1.8 100 >1000 53 >1000 100 68 ± 11 100 178 ± 23 100 >1000 60 NA 0
11 1000 ± 20 100 300 ± 30 100 71 ± 10 100 700 ± 89 100 760 ± 80 100 710 ± 70 100 2200 ± 200 100 550 ± 60 100
12 1.2 ± 0.2 100 70 ± 10 100 40 ± 10 100 520 ± 50 38 45 ± 5 100 65 ± 12 76 330 ± 57 100 390 ± 25 73
13 0.5 ± 0.01 100 1.5 ± 0.1 100 2.0 ± 0.02 100 2.0 ± 0.2 100 1.2 ± 0.2 100 1.4 ± 0.1 100 2.4 ± 0.3 100 1.9 ± 0.2 100
14 0.4 ± 0.01 100 0.7 ± 0.01 100 30 ± 3.9 100 6.7 ± 1 100 5 ± 1 100 2.1 ± 0.6 100 18 ± 2 100 8.1 ± 1.5 100
15 0.01 100 0.01 100 3.3 ± 0.3 100 0.8 ± 0.1 100 0.4 ± 0.02 100 0.2 ± 0.04 100 2.2 ± 0.5 100 1 ± 0.3 100
a IC is the peptide at 50% fic (N = 4). % BE the of [125 α-MSH at 10 μM. means that 0% of [125 -MSH
a

IC50 is the concentration of peptide at 50% specific binding (N = 4). % BE is the percentage of [125I]NDP-α-MSH displacement at 10 μM. NB means that 0% of [125I]NDP-α-MSH displacement was observed at 10 μM. EC50 is the effective concentration of peptide that could generate 50% maximal intracellular cAMP accumulation (N = 4). % max effect is the percentage of cAMP produced at a ligand concentration of 10 μM, in relation to MT-II. NA indicates 0% cAMP accumulation observed at 10 μM. The peptides were tested over a range of concentrations from 10−10 to 10−5 M. Compounds 1 and 11–15 were previously published data and are included for comparison.