Table 1.

Previous 11β-HSD1 inhibitors reported by the group [15,16] ^a,b.

Compound	hHSD1 IC50 (nM)	HEK hHSD2 % inh 10 µM or IC50 c	HLM % Parent d	mHSD1 IC50 (nM)	MLM % Parent d
1	86	88%	74	ND	ND
2	19	1–10 µM	27	ND	ND
3	29	0.1–1 µM	94	81	93

^a See Experimental section for further details; ^b Percentage inhibition was determined relative to a no inhibitor control; ^c HEK293 cells stably transfected with the full-length gene coding for human 11β-HSD2 were used; ^d The microsomal stability of each compound was determined using either human or mouse liver microsomes (HLM or MLM).