. Author manuscript; available in PMC: 2016 Jun 3.

Published in final edited form as: Tetrahedron Lett. 2015 Jun 3;56(23):3060–3065. doi: 10.1016/j.tetlet.2014.12.022

Table 2.

Competitive binding of compounds 11, 12, 13, and oligomers 5 to hMC4R.

Compound	Run	K_i^a (nM)	n^b
11		nb^c	1
12^d		350±28	4
13^e		560±110	5
5^e	1	190±24	6
5^e	5	270±31	7
5^e	10	200±32	5

The K_i was calculated using the equation K_i = IC₅₀/(1+([ligand]/K_d)) where [ligand] = [10] = 20 nM and K_d = 27 nM.

The value of K_i given represents the average of n independent competition binding experiments, each done in quadruplicate.

Compound 11 was unable to inhibit the binding and uptake of probe 10 in the concentration range tested.

K_i calculated based on [12], taken from ref 44.

K_i calculated based on [MSH4].