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. 2013 Oct;347(1):154–163. doi: 10.1124/jpet.113.206672

TABLE 2.

Inhibition constants (Ki) of enzymes involved in nucleotide biosynthesis for MTX and its polyglutamates (Allegra et al., 1985a,b; Drake et al., 1987; Baram et al., 1988; Sant et al., 1992)

Ki MTX-PG1 MTX-PG2 MTX-PG3 MTX-PG4 MTX-PG5
µM
DHFR 11.0 × 10−5 17.0 × 10−5 8.0 × 10−5 8.0 × 10−5
TS 13.0 0.17 0.14 0.13 0.047
AICART 143.9 5.47 0.56 0.056 0.057
GART 80 57 7.1 5.1 2.5
ATase ND 550

ND, no inhibition was detected.