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. 2019 Sep 6;39(9):BSR20191874. doi: 10.1042/BSR20191874

Table 1. Inhibition constants (Ki,app), Hill coefficients (h) and apparent dissociation constants derived from DSF experiments (KD,app) for wild-type NQO1 and the variants p.R139W and p.P187S.

Inhibitor Wild-type NQO1 p.R139W p.P187S
Ki,app
Dicoumarol 1.15 ± 0.51 nM 2.98 ± 1.04 nM 10.95 ± 1.11 nM2
Nicotinamide 14.01 ± 4.34 mM 13.55 ± 3.22 mM nd
Resveratrol 375 ±129 μM nd nd
Hill coefficient (h)
Dicoumarol 0.56 ± 0.09 0.51 ± 0.09 Inactive
Dicoumarol + excess FAD 0.47 ± 0.091,2 0.60 ± 0.042 0.48 ± 0.022
Resveratrol 0.89 ± 0.08 0.85 ± 0.12 nd
Nicotinamide 0.91 ± 0.06 0.92 ± 0.05 nd
KD,app
Dicoumarol 54 ± 4 nM 66 ± 11 nM 1100 ± 280 nM
Nicotinamide 6.0 ± 0.9 mM 18.2 ± 5.2 mM nd

h is the mean value from three separate linear Hill plots ± the standard deviation of this mean.

1

Previously reported and included here for comparison [39].

2

In excess FAD (10×[active site]).

nd, not determined.