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. 2021 Mar 6;48:101206. doi: 10.1016/j.molmet.2021.101206

Table 1.

Binding affinities of melanocortin ligands in cloned murine and human melanocortin receptors.

Peptide Murine receptors (nM)a
 Human receptors (nM)
MC1R MC3R MC4R MC5R MC1R MC3R MC4R MC5R
α-MSH 3.68 [165] 6.67(r) [166]
9.4(r) [167]
30.2 [168]
52(r) [169]		 9.17(r) [167]
61.2(r) [166]		 62.5 [170]
∼80 [171]		 0.0334 [172]
0.092 [173]
0.230 [174]
0.321 [175]
1.5 [176]
3.9 [177]
5.97 [178]		 15.5 [175]
19 [177]
20.7 [172]
21.2 [166]
31.5 [174]
46 [176]
50.04 [178]		 19 [177]
26 [176]
38.7 [178]
41.4 [175]
522 [166]
641 [179]
900 [174]		 120 [177]
150 [176]
332 [175]
557 [178]
928 [180]
7160 [174]
8240 [172]
β-MSHb 34.6(r) [166] 27.2(r) [166] 0.449 [173]
0.864 [175]
1.17 [172]		 13.4 [172]
15.1 [166]
23.2 [175]		 19.9 [175]
76 [179]
387 [166]		 306 [175]
1750 [180]
14,400 [172]
β-MSH(5–22) 19.4 [168] 212 [170] 2.29 [181] 39.46 [181] 22.74 [181] 301.5 [181]
β-MSH(1–22) 0.89 [182] 10.64 [182] 8.18 [182] 76.90 [182]
γ2-MSH 6.7 [168]
44(r) [169]		 1270 [170] 11.2 [172]
20.8 [175]		 17.7 [172]
57.2 [175]
72 [183]		 770 [183]
6250 [175]
100,000 [179]		 2500 [183]
3250 [175]
>100,000 [172]
ACTH(1–24) 8.15(r) [166] 35.6(r) [166] 32.8 [166] 755 [166]
ACTH(1–39) 21.1 [168] 236 [170]
∼300 [171]		 0.170 [173]
2.50 [172]		 86.9 [172] 693 [179] 929 [180]
17,000 [172]
Setmelanotide 2.7(r) [185] 5.5 [184],e
3.9 [175,185]		 10 [175,185]
18 [184],e 		2.1 [175,185]
5.0 [184],e 		430 [175,185]
1910 [184],e
Bremelanotide 3.4 [184],e 72.07 [186]
220 [184],e 		10 [187]
19.25 [186]
29 [184],e 		166.8 [186],e
190 [184]
MTII 0.22 [188]c 1.85 [188]c
4.77(r) [167]
67.8(r) [166]		 1.74(r) [167]
6.22(r) [166]
0.50 [188,189]c 		28.4 [188]c 0.20 [184],e
0.268 [175]
0.36 [177]
0.686 [174]
6.4 [176]		 1.6 [190]
3.1 [177]
20 [184],e
34.1 [174]
24.0 [175]
52.6 [166]
53 [176]		 0.07 [190]
0.18 [177]
0.25 [176]
1.5 [184],e
2.66 [175]
6.60 [174]
39.7 [166]		 0.89 [190]
1.2 [177]
17 [176]
23 [184],e
23.1 [175]
46.1 [174]
Ac-His-DPhe-Arg-Trp-NH2 388 [191] 60%@100 μM [191] 214 [191] 615 [178] >10 μM [178] 1153 [178] >10 μM [178]
NDP-MSH 0.29 [188]
0.79 [165]
0.31 [191]		 0.479(r) [166]
1.19(r) [167]
1.4 [168]
1.45 [188]
4.18 [191]
10(r) [169]		 0.417(r) [166]
0.88 [188,189]
1.09 [191]
3.14(r) [167]		 1.1 [170]
27.6 [188]		 0.023 [173]
0.0231 [172]
0.046 [176]
0.109 [175,192]
0.39 [193]
0.51 [178]		 0.224 [172]
0.319 [166]
0.469 [174]
0.680 [175]
0.78 [176,193]
1.17 [178]
2.9 [183]		 0.30 [176]
0.620 [175]
1.16 [178]
1.6 [193]
1.96 [166]
2.16 [179]
2.93 [174]
3.3 [183]		 0.27 [193]
0.48 [176]
0.86 [178]
0.89 [183]
0.891 [175]
2.39 [172]
5.18 [180]
5.50 [174]
SHU9119 0.879(r) [167]
1.68(r) [166]		 0.238(r) [167]
0.38 [189]c
0.583(r) [166]		 0.62 [177]
0.714 [170]		 0.23 [177,194]
1.20 [174]
1.65 [166]		 0.06 [194]
0.07 [177]
0.360 [174]
0.689 [166]		 0.065 [177]
0.09 [194]
1.12 [174]
Agoutid 2.6(B16F10) [195] 190 [195] 54 [195] 1200 [195] 23 [195] 112 [196]
140 [195]		 12 [196]
70 [195]		 >1000 [195]
AgoutiYY 15.3 [197] 14.1 [197] 1.8 [197]
AGRP 2.8 [198]c 0.66 [189]c
3.0 [198]c 		None [199]c 1.1 [200]
4.5 [201]
11.2 [199]c 		0.5 [200]
3.5 [201]
9.0 [199]c
24.7 [202]c 		25.6 [199]c
>40 [200]
a

Values labelled with a (r) represent data from cloned rat receptors. Unlabelled numbers represent mouse receptors.

b

Affinity β-MSH values were split depending on the sequence used. If a sequence was not provided in the paper, values are listed in the β-MSH row.

c

The radiolabels [125I]MTII, [125I]SHU9119, and [125I]AGRP were used at their respective ligands as indicated in place of [125I]NDP-MSH.

d

A mouse cell line natively expressing the MC1R was used.

e

Values shown are IC50 values converted from pKi and pIC50 values reported in the source publication.