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. Author manuscript; available in PMC: 2015 Nov 15.
Published in final edited form as: Bioorg Med Chem. 2014 Oct 2;22(22):6360–6365. doi: 10.1016/j.bmc.2014.09.055

Table 2. Binding affinities of monovalent and bivalent ligands for hMC4R.

ligand Structure aLogEC50 bEC50 (nM) Hill coefficient
1 Ac-(Pro-Gly)6-SHU9119-NH2 -8.40 ± 0.06 4.0 1.1
2 Ac-(Pro-Gly)9-SHU9119-NH2 -8.09 ± 0.05 8.1 0.8
3 Ac-(Pro-Gly)12-SHU9119-NH2 -7.88 ± 0.17 13 1.1
4 Ac-PEGO-(Pro-Gly)3-PEGO-SHU9119-NH2 -8.43 ± 0.06 3.7 0.9
5 Ac- PEGO-SHU9119-NH2 -7.60 ± 0.51 24 0.6
6 Ac- PEGO-PEGO-SHU9119-NH2 -6.39 ± 0.46 400 0.8
7 Ac-SHU9119-(Pro-Gly)6-SHU9119-NH2 N.D N.D -
8 Ac-SHU9119-(Pro-Gly)9-SHU9119-NH2 -8.81 ± 0.02 1.6 2.2
9 Ac-SHU9119-(Pro-Gly)12-SHU9119-NH2 -8.71 ± 0.02 2.0 3.0
10 Ac-SHU9119-PEGO-(Pro-Gly)3-PEGO-SHU9119-NH2 -8.67 ± 0.02 2.2 1.9
11 Ac-SHU9119-PEGO-SHU9119-NH2 -8.74 ± 0.06 1.8 2.2
12 Ac-SHU9119-PEGO-PEGO-SHU9119-NH2 -8.73 ± 0.02 1.9 1.9
13 Ac-MSH(7)-(Pro-Gly)6-SHU9119-NH2 -8.39 ± 0.12 4.1 0.7
14 Ac-MSH(7)-(Pro-Gly)9-SHU9119-NH2 -8.71 ± 0.08 2.0 0.8
15 Ac-MSH(7)-(Pro-Gly)12-SHU9119-NH2 -8.80 ± 0.04 1.6 2.0
16 Ac-MSH(7)-PEGO-(Pro-Gly)3-PEGO-SHU9119-NH2 -8.86 ± 0.03 1.3 2.4
17 Ac-MSH(7)-PEGO-SHU9119-NH2 -8.73 ± 0.02 1.4 2.7
18 Ac-MSH(7)-PEGO-PEGO-SHU9119-NH2 -8.77 ± 0.02 1.7 2.7
19 Ac-(Pro-Gly)6- MSH(7)-NH2 82 ± 12c
20 Ac-(Pro-Gly)9- MSH(7)-NH2 236 ± 24c
21 Ac-(Pro-Gly)12- MSH(7)-NH2 188 ± 25c
22 Ac-MSH(7)-(Pro-Gly)6- MSH(7)-NH2 11 ± 2c
a

The logEC50 ± SEM are logarithmic values determined from the nonlinear regression analysis of data collected from 4 independent concentration range.

b

Determined from Dissociation Enhanced Lanthanide FluoroImmuno Assay (DELFIA) using optimized 10 nM standard agonist Eu-DTPA-NDP-α-MSH chelate.