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Table 3 IC50 values on NTS and adult S. mansoni, toxicity on L6 and MRC5-cells and selectivity of the 11 Stasis Box lead molecules. Cytotoxic concentration (CC50) and selectivity index (SI) are compared to the mean IC50 values measured on NTS and adult S. mansoni in standard and albumin-enriched medium (45 g/l) over 72 h with 11 Stasis Box lead compounds

From: Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni

Compound

MMV ID

NTS IC50 (μM)a

Adult IC50 (μM)a

Adult IC50 (μM) with albumina

L6 cells

MRC5 cellsd

 

24 h

48 h

72 h

24 h

48 h

72 h

24 h

48 h

72 h

CC50 (μM)

SI

CC50 (μM)

SI

MMV690732

29.5

6.3

3.5

4.9

2.9

2.5

62.8

181.0

54.1

2.3

0.9

1.9

0.7

MMV690596

1.1

1.3

0.6

1.0

2.1

2.0

27.5

14.4

11.0

3.5

1.7

1.9

0.9

MMV003452

4.4

2.2

1.2

1.7

3.0

2.7

22.6

12.0

7.5

3.7

1.4

1.9

0.7

MMV690599

10.5

3.5

1.5

2.5

3.3

2.6

23.6

19.1

15.9

3.4

1.3

2

0.8

MMV690466

14.6

3.8

2.1

2.9

2.3

2.0

18.1b

89.7

47.6

1.6

0.8

8.4

4.3

MMV690787

38.4b

8.1

6.3

7.9

7.2

3.1

39.5

14.4

13.3

na

na

0.1

0

MMV690684

4.0c

3.1c

0.7

4.9

4.7

3.7

76.8

14.4b

7.7

7.0

1.9

7

1.9

MMV690646

3.0c

1.1

0.9

3.7

2.2

2.2

32.0

121.8

33.6

na

na

0.2

0.1

MMV690765

914.4b

> 1c

0.5b

4.2

3.4

2.9

651.7

225.9b

123.5b

11.8

4.1

0.7

0.3

MMV690534

11.8

14.3c

7.2c

17.4

19.3

7.5

na

na

na

74.5

15.0

12.4

2.5

MMV001539

12.7

11.0c

1.7

28.2

12.3

7.0

nd

nd

nd

2.9

0.4

16

2.1

  1. Abbreviations: na not applicable. nd not done
  2. ar-values ranged between 0.7 and 1.0
  3. bThese values are based on one replicate only because of an r-value < 0.70 was obtained for the second replicate
  4. cThe IC50 values obtained in each of the two replicate differed more than 5.5-fold
  5. dThe CC50 values on MRC5 cells were provided by MMV