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. 2023 Jan 24;18(4):e202200580. doi: 10.1002/cmdc.202200580

Table 1.

β‐D‐Glucuronidase inhibition efficacy by 36.

Inhibitor

IC50 [μM] EcGUS[a]

IC50 [μM] AcGH79[a]

IC50 [μM] HPSE[b]

Selectivity factor[c]

1 [d]

0.5±0.1

0.033±3 ⋅ 10−3

>100

N/A

3

>100

21±7

>100

N/A

4

>100

0.156±6 ⋅ 10−3

5±2

20

5

>100

0.167±9 ⋅ 10−3

1.5±0.7

67

6

0.43±0.07

1.43 ⋅ 10−3±0.08 ⋅ 10−3

0.2±0.2

2

[a] 4‐MU fluorogenic substrate assay. [b] In gel competitive ABPP‐based assay. Reported values are mean±S.D. of three technical replicates. [c] Calculated as ratio IC50 EcGUS/IC50 HPSE. [d] Reported values are taken from the literature.[ 21 , 22 ]