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. Author manuscript; available in PMC: 2020 Mar 20.
Published in final edited form as: ACS Chem Neurosci. 2018 Aug 13;10(3):1055–1065. doi: 10.1021/acschemneuro.8b00346

Table 2.

Comparison of Inhibition Constants (Ki) and 50% Maximum Concentration (EC50) Values for α-MSH and RM-493 in Radioligand Binding and Intracellular cAMP Production Assays27

mutation Ki (nM) EC50 (nM)
α-MSH RM-493 α-MSH RM-493
WT 26 ± 7.0 0.71 ± 0.16 30 ± 7.5 1.5 ± 0.38
SerS8Cys 53 ± 12 1.7 ± 4.3 670 ± 90 46 ± 8.0
Ile102Thr 210 ± 94 2.2 ± 0.21 5800 ± 850 150 ± 57
Ser127Leu 160 ± 40 3.3 ± 0.13 640 ± 190 17 ± 6.0
Gly252Ser 160 ± 66 2.3 ± 0.30 210 ± 45 13 ± 2.0