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Table 5 (a) Cross-resistance profile of FNDR-20123 (b) Hypersensitivity profile of FNDR-20123

From: Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria

(a)

Mutated locus

Mutations (amino acid changes)

FNDR-20123

IC50 (nM)

Fold shift IC50 rel. Dd2

Dd2

Wild type

N/A

17.50

1.0

Dd2 DDD107498

PfeEF2

Y186N

20.86

1.2

Dd2 390048

Pfpi4k

S743T

18.27

1.0

Dd2 DSM265

Pfdhodh

G181C

17.83

1.0

Dd2 GNF156

Pfcarl

Ile1139Lys

18.45

1.1

Dd2 ELQ300

PfcytB

Ile22Leu

13.49

0.8

(b)

FNDR-20123

IC50 (nM)

Fold shift IC50 rel. NF54

 NF54

25.27

1.0

 K1

19.05

0.75

 7G8

14.36

0.57

 TM90C2B

13.26

0.52

 Cam3.I (MRA1240)

22.06

0.87

 Dd2

17.50

0.69