Table 1 Confirmed hits from 6-day prophylactic assays of the reference compound library.

From: Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro

Synonyms

Class or targetREF

Schizont net growth area

Hypnozoite quantity

Nuclei quantity

EC50 (μM)

Max Inh (%)

EC50 (μM)

Max Inh (%)

CC20 (μM)

Max Inh (%)

UCT943

PI4K41

0.00175

100

0.00427

100

> 10.0

15.6

CC_642944

PI4K41

0.00476

101

101

98.9

> 10.0

1.28

DDD107498 (M5717)

eEF242

0.00257

101

0.0104

100

> 10.0

0.326

KAF156

IZP24

0.0141

103

0.0329

105

> 10.0

4.83

Clindamycin

Antibiotic43

0.00597

79.5

> 50.0

53.8

> 50.0

5.01

Methotrexate

Folic acid antagonist44

0.0428

99.1

> 10.0

12.9

> 10.0

6.07

P218

DHFR45

0.0511

101

> 10.0

5.15

> 10.0

9.08

ELQ-300

Cytochrome bc146

0.0576

97.9

> 1.11

71.9

> 10.0

7.2

DSM265

DHODH47

0.126

100

> 3.07

37.4

> 3.07

9.06

DSM421

DHODH48

0.325

98.8

> 10.0

61.2

> 10.0

4.76

AZ412

V-type H+-ATPase49

0.686

99.7

> 3.33

54.8

> 10.0

2.49

Cycloheximide

Antifungal50

1.39

99.6

> 3.33

85.7

> 10.0

8.17

AN13762 (AN762)

Oxaborole, CPSF351

1.63

99.7

> 1.11

93.2

> 10.0

6.64

Chlorproguanil

DHFR52

> 1.11

98.1

> 10.0

26

> 10.0

9.62

NPC-1161B

8AQ53

> 0.370

91.9

> 10.0

41.3

> 10.0

6.73

Pamaquine

8AQ54

ND

87.1

> 3.33

27.1

> 10.0

1.25

N-Desethylamodiaquine

4AQ55

> 3.33

74.5

> 10.0

15.8

> 10.0

15.3

Trans-Mirincamycin

Antibiotic56

ND

72.5

> 10.0

47.4

> 10.0

4.62

Cis-Mirincamycin

Antibiotic56

ND

69.3

> 10.0

19.5

> 10.0

13.2

Doxycycline hydrochloride

Antibiotic57

> 0.370

68.3

> 10.0

36.7

> 10.0

3.57

Amodiaquine

4AQ55

0.0141

65.6

> 10.0

16.3

> 10.0

18.6

Azithromycin

Antibiotic58

> 0.370

63.3

> 10.0

24.6

> 10.0

10.7

Artemether

Artemisinin derivative59

ND

60.4

> 10.0

35.2

> 10.0

11.4

Tetracycline

Antibiotic57

ND

56.7

> 10.0

19.9

> 10.0

3.64

AQ-13

4AQ60

ND

56.1

> 10.0

29.4

> 10.0

6.97

  1. All EC50’s, CC20’s, and Maximum Inhibition (Max Inh) values are from the highest quality independent experiment. RCL, Reference Compound Library; PI4K, phosphatidyl inositol 4-kinase; eEF2, elongation factor 2; IZP, imidazolopiperazine; DHFR, dihydrofolate reductase; DHODH, dihydroorotate dehydrogenase; CPSF3, cleavage and polyadenylation specificity factor subunit 3; 8AQ, 8-aminoquinoline; 4AQ, 4-aminoquinoline. Included are activity values for selective compounds; activity data for selective and nonselective compounds, as well as structures, can be found in Supplementary Table S1 online.
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