. 2018 Oct 4;3(10):12658–12678. doi: 10.1021/acsomega.8b01237

Table 7. Antagonism of KOR in the βarrestin2-KOR Enzyme Fragment Complementation Assay (DiscoveRx) and cAMP Cisbio Assay^a^,^b.

	βarrestin2 recruitment		inhibition of cAMP accumulation
compound	IC₅₀ (nM)	Imax (% 120)	IC₅₀ (nM)	Imax (% 120)
120	2.0 ± 0.3	100	4.0 ± 0.8	100
28	794 ± 50	92 ± 1	2220 ± 830	122 ± 13
39	4200 ± 940	77 ± 3	13100 ± 6000	105 ±3
40	2220 ± 540	76 ± 2	12100 ± 4400	100 ± 1
43	NC	(10* ± 15)	NC	(23 ± 5)
54	NC	(35* ± 4)	NC	(16 ± 6)

Data are the mean ± SEM of N = 3 Assays Performed in Duplicate (Figures 1 and 2).

NC: not converged; (% inhibition at 30 μM). 120 (norbinaltorphimine, nor-BNI) is the reference KOR antagonist.

Table 7. Antagonism of KOR in the βarrestin2-KOR Enzyme Fragment Complementation Assay (DiscoveRx) and cAMP Cisbio Assaya,b.