. Author manuscript; available in PMC: 2016 Dec 27.

Published in final edited form as: J Am Chem Soc. 2016 May 18;138(21):6754–6764. doi: 10.1021/jacs.6b00360

Table 3.

Agonist Activity of Synthetic Analogs at hMOR as Determined in G Protein BRET Assays

Compound	Structure	EC₅₀ ± SEM (% efficacy) (µM) ^a
(-)-mitragynine		0.339 ± 0.178 (34%)
(+)-mitragynine		3.34 ± 1.1 (18%)
1		0.681 ± 0.379 (29%)
2		>50
11		0.219 ± 0.071 (38%)
3		12 ± 7.6 (59%)

Agonist activity at hMOR indicated by EC₅₀ values, maximal efficacy (E_max) relative to DAMGO in parentheses; All data points represent mean ± SEM (µM) of n ≥ 3.