Table 3 Selectivity of SapM inhibitors towards phosphatases. Inhibition of selected compounds towards mycobacterial secreted phosphatases SapM, MptpA and MptpB, and human phosphatases PTP1B and VHR.

From: Discovery of uncompetitive inhibitors of SapM that compromise intracellular survival of Mycobacterium tuberculosis

Compound number

IC50 (µM)

SapM

MptpA

MptpB

PTP1B

VHR

1

6.3 ± 1.0

19.8 ± 1.0

 > 100

 > 100

 > 100

2

9.3 ± 1.1

55.2 ± 1.1

 > 100

 > 100

 > 100

3

19.8 ± 1.1

 > 100

 > 100

–

–

4

ND

–

–

–

–

5

73.9 ± 1.2

–

–

–

–

6

41.9 ± 1.1

 > 100

 > 100

–

–

13

8.2 ± 1.0

16.7 ± 1.0

 > 100

 > 100

 > 100

14

14.5 ± 1.0

23.7 ± 1.1

 > 100

–

–

15

78.42 ± 2.7

–

–

–

–

29

63.0 ± 1.5

 > 100

 > 100

–

–

  1. IC50 values are mean ± SD of two independent experiments.
  2. ND not determined as compound precipitates at concentrations > 100 µM.
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