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. Author manuscript; available in PMC: 2015 Jan 3.

Published in final edited form as: Expert Opin Investig Drugs. 2013 Dec 13;23(2):227–241. doi: 10.1517/13543784.2014.856879

Table 4.

Binding and functional assay data of cyclic ligands at opioid receptors (OR).


Compound number	GPI			MVD		GPI/MVD	OR binding affinity			Binding ratio

	IC₅₀ (nM)	K_e^μ (nM)	K_e^κ(nM)	IC₅₀ (nM)	K_e^δ (nM)	IC₅₀ ratio	K_i^μ(nM)	K_i^δ (nM)	K_i^κ (nM)	K_i^μ/K_i^δ/K_i^κ
49	1.07	–	–	1.11	–	1/1	0.496	2.29	0.45	1/5/1
50	0.457	–	–	0.884	–	1/2	0.354	2.36	0.86	1/7/2
51	1.81	–	–	0.352	–	5/1	0.504	0.525	1.01	1/1/2
52	1.36	–	–	0.122	–	11/1	0.586	0.776	0.89	1/1/2
53	1.34	–	–	3.72	–	1/3	0.876	6.07	1.42	1/7/2
54	0.394	–	–	1.95	–	1/5	0.641	1.79	0.88	1/3/1
55	0.586	–	–	0.0530	–	11/1	0.412	0.202	0.68	1/0.5/1.6
56	0.812	–	–	0.115	–	7/1	0.282	0.306	0.68	1/1/2
57	–	71.0	151	–	277	–	14.4	35.9	29.5	1/2/2
58	1.41	–	–	23.1	–	1/16	0.143	2100	22.3	1/11400/156
59	2.2	–	–	6.2	–	1/2.8	0.23	15.2	16.2	1/66/70
60	0.31	–	–	1.4	–	1/4.5	0.57	50.0	20.9	1/88/37
61	0.89			4.7		1/5.3	0.79	3.98	98.5	1/5/125
62	8.3	–	–	7.0	–	1.2/1	0.26	309	56.1	1/1190/216
63	4.35	–	–	1.5	–	2.9/1	0.26	16.0	14.4	1/62/55
64	1.01	–	–	4.4	–	1/4.4	0.94	39.2	11.5	1/42/12
65	0.65	–	–	1.5	–	1/2.3	2.92	5.03	> 10,000	1/2/> 3420
66	76.0	–	–	64 (IC₂₅)	–	–	0.61	38.60	ND	1/64/–
67	1.45	–	–	3.1	–	1/2.1	0.43	7.46	1.12	1/17/3
68	49.0	–	–	1000	–	1/20	2.62	56.9	ND	1/22/–
69	0.78 (IC₃₅)	–	–	1.16	–	–	0.93	3..18	11.1	1/3/12
70	0.32	–	–	0.42	–	1/1.3	0.15	0.60	118	1/4/787