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. 2022 Mar 23;26(9):1200–1211. doi: 10.1177/24725552211026261

Table 1.

Confirmation and Selectivity of nsp14 Screening Hits.

Compound SPR KD (µM) of Nsp14 IC50 (µM)a
Nsp 14 G9a BCDIN3D ALKBH5 SETD3 METTL3-14
SS148 0.05 0.07 ± 0.006 NI 0.03 ± 0.002 NI NI 0.9
WZ16 NA 0.19 ± 0.04 NI 1.7 NI 3.4 3.4
DS0464 1.6 1.1 ± 0.2 NI 46 ± 9 NI NI NI
DS0466 2.4 3.4 ± 1.4 NI >50 NI NI NI
JL27-56A1 0.2 0.26 ± 0.13 NI 19 NI 23 10
Compound 8 18.9 95 ± 6 NI NI NI NI NI
SAH 0.14 0.13 ± 0.03 NA NA NA NA NA
MTTR025495 6.2 17 ± 2 NA NA NA NA NA

The screening hits were tested for binding to nsp14 by SPR and for inhibition of MTase activity of nsp14 and selected MTases by activity assays. All values are from experiments presented in Figure 3andSupplemental Figures S7, S10, S11, S12, S13, and S14. NA, not assessed; NI, no inhibition. aIC50 values are presented as the mean ± standard deviation (n = 3).