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. 2008 Aug 13;64(Pt 9):977–984. doi: 10.1107/S0907444908022348

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

Inhibitor pcDHFR Rat DHFR Rat DHFR/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