Off target protein and potency: OPRD1: 24 nMOPRM1: 53 nMUTS2R: 4,000 nM
Potency assay (off target):
Measured using [3H]-diprenorphine as radioligand in binding assay (OPRD1, OPRM1) reported in Bioorg. Med. Chem. Lett., (2005) 15:10:2647 and confirmed in subsequent publications. Binding affinity to human urotensin-2 receptor reported in Bioorg. Med. Chem. Lett., (2008) 18:13:3716.
Selectivity against non-family targets:
CYP2D6 IC50 = 26 nM