Table 4.

In vitro PK properties of selected compounds

Compound#	MLMSa (%)	HLMSb (%)	CYP3A4 % INHc	Solubilityd (µM)
morpholinyl compounds
MBX 2319	0	0	12	12
20f	0	8	29	50
20r	5	21	49	25
(2-methoxyethyl)piperazinyl compounds
19e	0	0	18	50
21a	3	0	14	≥ 100
21f	17	N.D.	42	≥ 100
21g	13	20	48	≥ 100
2,6-dimethylmorpholinyl compounds
22a	19	53	0	≥ 100
22d	66	59	0	100
22e	72	76	59	12
22f	0*	37	61	50
22g	0*	90	66	12.5
22i	49	100	90	25
22k	90	90	9	100

^aMLMS, murine liver microsome stability, % remaining after 60 min at 37 °C in the presence of NADPH.

^bHLMS, human liver microsome stability, % remaining after 60 min at 37 °C in the presence of NADPH.

^cCYP3A4 INH, percent inhibition produced by 3 µM compound.

^dSolubility, maximum solubility in water as determined using a nephelometric assay³²

^*NADPH independent consumption