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. Author manuscript; available in PMC: 2009 Jan 8.
Published in final edited form as: Acta Crystallogr D Biol Crystallogr. 2008 Aug 13;64(Pt 9):977–984. doi: 10.1107/S0907444908022348

Table 1.

Enzyme inhibition (IC50 nM) against DHFR for selected inhibitors (Fig. 1) (Chan et al, 2005; Rosowsky et al, 2004)

Inhibitor pcDHFR rat DHFR rat/pcDHFR Selectivity Ratio
TMP 13000 180000 13.8
PTX 13 3.3 0.26
PT684 1.1 1500 1363
PT682 1.0 580 580
PT684a 31 14 1.3
PT653 79 3000 37.9