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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 2.

Binding affinity and functional activities at ORs.


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

	IC₅₀ (nM)	IC₅₀ (nM)	IC₅₀ ratio	K_i^μ (nM)	K_i^δ (nM)	K_i^κ (nM)	K_i^μ/K_i^δ/K_i^κ
16	0.226	0.319	1/1.4	0.293	9.99	6.93	1/34/24
17	0.717	0.211	3.4/1	0.443	0.389	1.53	1/0.9/3.5
18	0.542	0.182	3/1	0.247	0.704	3.77	1/3/15
19	0.984	4.60	1/4.7	0.948	102	1.39	1/108/1.5
20	254	781	1/3	1.69	19200	4230	1/11360/2503
21	1.41	23.1	1/16	0.143	2100	22.3	1/14685/156
22	0.591^*	1.07	–	3.41	13.9	1.56	1/4/0.5
23	0.376	15.2	1/40	0.653	13.5	0.087	1/21/0.13
24	0.502	0.377	1.3/1	0.322	0.435	1.18	1/1.4/3.7
25	3.64	30.3	1/8	20.8	17.8	–	1.2/1/–
26	22.0	79.7	1/4	28.1	7.1	–	4/1/–
MF/Morphine	29.3	155	1/5	9.77	112.2	–	1/11/–
28	318	4800	1/15	19.8	> 1000	–	1/> 50/–
29	9.57	35.4	1/3.6	0.47	> 1000		1/> 2127/–
30	0.45	0.64	1/1.4	0.00055	132	–	1/24044/–
31	7.71	15.3	1/2	0.79	> 1000	–	1/> 1266/–
32	872	2040	1/2.3	22.3	> 1000	–	1/> 45/–
33	1.53	1.63	1/1.1	0.93	> 1000		1/> 1075/–
34	–	–	–	–	0.56	–	–/–/–
35	246	11.4	21.6/1	–	–	–	–/–/–

^*

Partial agonist.