Table 1 IC50 values of aspartyl protease inhibitors against B. divergens

From: Babesia divergens host cell egress is mediated by essential and druggable kinases and proteases

 

Wild-type IC50 (±s.d.) (µM)

ASP2 (high Shld1) IC50 (±s.d.) (µM)

ASP2 (low Shld1 = knockdown) IC50 (±s.d.) (µM)

ASP3 (high Shld1) IC50 (±s.d.) (µM)

ASP3 (low Shld1 = knockdown) IC50 (±s.d.) (µM)

CWHM-0000032

0.891 (±0.307)

0.320 (±0.212)

0.478 (±0.288)

0.362 (±0.129)

0.246 (±0.095)

CWHM-0000033

4.03 (±1.90)

1.57 (±0.17)

1.63 (±0.94)

1.39 (±0.26)

0.539 (±0.358)

CWHM-0000099

>25

11.8 (±0.8)

3.99 (±3.15)

16.3 (±3.7)

2.85 (±1.52)

CWHM-0000117

6.81 (±3.08)

2.66 (±0.55)

2.56 (±1.32)

3.17 (±0.61)

1.13 (±0.50)

CWHM-0000166

8.80 (±3.18)

2.89 (±1.27)

1.15 (±0.70)

2.76 (±0.96)

0.337 (±0.157)

CWHM-0000047

19.5 (±5.3)

18.5 (±12.9)

6.32 (±5.84)

16.9 (±9.0)

8.47 (±5.35)

CWHM-0000579

12.6 (±6.6)

7.49 (±4.73)

11.1 (±6.5)

9.12 (±6.12)

7.32 (±6.48)

CWHM-0000162

13.3 (±9.4)

7.15 (±6.45)

6.47 (±5.35)

8.00 (±5.06)

6.41 (±6.74)

SLU-0010620

19.8 (±5.3)

10.1 (±3.4)

4.67 (±3.06)

14.1 (±2.6)

10.0 (±5.4)

SLU-0010622

10.9 (±3.3)

6.38 (±3.27)

1.89 (±2.78)

8.04 (±3.36)

5.49 (±4.29)

CWHM-0000068

16.6 (±7.6)

15.7 (±12.6)

8.02 (±0.89)

13.3 (±2.9)

9.88 (±4.84)

CWHM-0000116

>25

>25

18.8 (±8.2)

20.3 (±11.3)

21.4 (±10.2)

CWHM-0000123

9.46 (±3.66)

8.39 (±4.39)

10.8 (±2.8)

11.2 (±8.7)

9.22 (±1.76)

CWHM-0000293

>25

>25

>25

>25

>25

CWHM-0000299

>25

>25

>25

>25

>25

CWHM-0000460

>25

12.3 (±10.2)

12.2 (±1.5)

12.4 (±5.6)

12.6 (±4.0)

CWHM-0000580

>25

>25

>25

>25

>25

CWHM-0000583

>25

14.2 (±9.5)

14.5 (±8.9)

13.8 (±5.1)

14.1 (±6.9)

CWHM-0000658

16.2 (±9.8)

12.6 (±11.9)

6.47 (±3.82)

9.35 (±3.77)

7.82 (±5.45)

SLU-0010621

25.7 (±12.3)

15.8 (±9.6)

8.64 (±4.98)

15.8 (±3.6)

18.6 (±13.4)

SLU-0010623

24.2 (±10.7)

6.37 (±3.46)

2.57 (±2.67)

13.4 (±7.2)

12.1 (±8.2)

SLU-0010624

18.5 (±5.7)

6.38 (±3.72)

5.76 (±6.77)

9.62 (±4.22)

9.30 (±6.24)

UCB7362

0.908 (±0.232)

1.21 (±0.76)

0.764 (±0.306)

0.113 (±0.021)

0.020 (±0.012)

WM382

0.0341 (±0.0064)

0.00775 (±0.0019)

0.00267 (±0.0014)

0.00695 (±0.0010)

0.00088 (±0.0005)

ML10

0.864 (±0.319)

0.794 (±0.072)

1.56 (±1.24)

0.682 (±0.256)

0.628 (±0.219)

Atovaquone

0.021 (±0.007)

0.020 (±0.005)

0.020 (±0.008)

0.021 (±0.006)

0.025 (±0.011)

  1. Activity of aspartyl protease inhibitors against WT and ASP2 and ASP3 knockdown parasite growth.