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. Author manuscript; available in PMC: 2015 Oct 7.
Published in final edited form as: J Med Chem. 2015 Aug 11;58(16):6359–6367. doi: 10.1021/acs.jmedchem.5b00102

Figure 2.

Figure 2

(a) Amino acid sequences for Ac-Nle4-c[Asp5,d-Nal(2′)7,Lys10]-NH2 (peptide 1) and N-methylated Ac-Nle4-c[Asp5,d-Nal(2′)7,Lys10]-NH2 analogues (peptides 2–32; the site of N-methylation is highlighted in bold. (b–e) Histograms showing the results for IC50 from binding assays (black bars) and EC50 from cAMP assays (light gray bars) at hMC1R, hMC3R, hMC4R, and hMC5R, respectively. Although IC50 and EC50 values on the y axis are in real number units, for convenient representation and comparison, log10 scaling is used on the y axis. The specific IC50 and EC50 values for each peptide are indicated above its corresponding histogram bar. Act% values (>0%) of the ligands for the cAMP assay are plotted in red with a second y dimension on the right. The location of the red spots demonstrates increased and decreased agonist activity. For more details, including the binding efficiency, refer to Tables 2 and 3. IC50, concentration of peptide at 50% specific binding (N = 4); EC50, effective concentration of peptide that was able to generate 50% maximal intracellular cAMP accumulation (N = 4).