TABLE 1 .

Physiochemical and biochemical assays for SMM-295

Assay	Species	Receptor	Parameter	Value	CB1/CB2	Efflux Ratio (B-A/A-B)
Binding	Human	CB1	Ki	379 ± 53 nM	31
	Human	CB2	Ki	12 ± 2.26 nM
cAMP inhibition	Human	CB1	EC50	1190 ± 22.1 nM	66
	Human	CB2	EC50	18.1 ± 1.45 nM
Protein binding (% bound)	Human			>99.9
	Mouse			>99.9
hERG (% inhibition)	Human		10 μM	4 ± 3
	Human		1 μM	<0.1%
Permeability	Human		Papp A →B	5.2 ± 0.4 × 10−6 cm/s		1.4
	Human		Papp B → A	7.1 ± 1.2 × 10−6 cm/s
	Human		Papp A → B (+ verapamil)	7.9 ± 0.1 × 10−6 cm/s		0.9
	Human		Papp B → A (+ verapamil)	6.7 ± 0.2 × 10−6 cm/s