Table 5. GAC versus GLS2 Selectivity of the Best 2-Sulfonylpyrimidine/2-Thiopyrimidine Derivatives.
IC50 (μM) [95% CI] |
|||
---|---|---|---|
cpd | GAC | GLS2 | enzymatic selectivity ratio (IC50 GLS2/IC50 GAC) |
C9 | 118 [92–162] | >200 | >1.7 |
C9.12 | 19 [14–24] | >200 | >10.5 |
C9.19 | 24 [21–29] | >200 | >8.3 |
C9.20 | 23 [12–41] | >200 | >8.7 |
C9.22 | 20 [17–24] | >200 | >10 |
C9.24 | 36 [21–56] | >200 | >5.5 |
C9.25 | 29 [26–33] | 106 [45–892] | 3.7 |
CB-839 | 0.034 [0.030–0.039] | >200 | >5882 |