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 |