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. Author manuscript; available in PMC: 2014 Sep 1.
Published in final edited form as: Arch Biochem Biophys. 2013 Jun 27;537(1):12–20. doi: 10.1016/j.abb.2013.06.011

Table 3.

Inhibition parameters for pyrazoles toward CYP2E1 oxidation of 4-nitrophenola

Inhibitor Inhibition
Mechanismb 		Kd1 (µM) Kd2 (µM) kcat2 (min−1)
Monocylic pyrazoles
  pyrazole Mixed, coop. substrate 140 (72 to 520) 98 (77 to 131) -
  3-methylpyrazole Mixed, coop. substrate 11 (8.3 to 16) 21 (13 to 35) 8.7 (7.0 to 10)
  4-methylpyrazole Mixed, coop. substrate 0.93 (0.72 to 1.2) 3.1 (2.1 to 5.1) 7.3 (6.0 to 8.7)
  3,5-dimethylpyrazolec - - - -
Bicyclic pyrazoles
  3-phenylpyrazole Competitive 19 (15 to 25) - -
  indazole Mixed, coop. substrate 0.13 (0.10 to 0.18) 0.35 (0.21 to 0.66) 11 (9.0 to 13)
  tetrahydroindazole Mixed, coop. substrate 1.0 (070 to 1.6) 2.7 (1.4 to 7.7) 6.6 (2.3 to 9.6)
a

95% confidence intervals shown in parentheses

b

Consult Table 1 and Scheme 2

c

No inhibition was observed for 3,5-dimethylpyrazole