. Author manuscript; available in PMC: 2011 Jun 24.

Published in final edited form as: J Med Chem. 2010 Jun 24;53(12):4768–4778. doi: 10.1021/jm100424m

Table 2.

Biological evaluations of IMPDH inhibitors

Compound	K_i^apphIMPDH1 (μM)	K_i^apphIMPDH2 (μM)	K_i^appmtIMPDH (μM)
1	0.033^a	0.007^a	62
3a	0.33^a	0.25^a	>100
3b	0.066^a	0.11^a	>100
3c	0.016^a	0.038^a	>100
4	0.52^b	0.38^b	>100
5a	0.35^c	0.17^c	>100
5b	0.66^c	0.31^c	>100
5c	0.52^c	0.18^c	>100
5d	0.82^c	0.44^c	>100
6	14	2.2	>100
7	0.077	0.034	>100
8	1.5	0.20	>100
9	0.070	0.044	1.5^d (2.2)^e

uncompetitive K_iu vs. NAD

uncompetitive K_iu vs. IMP.