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. Author manuscript; available in PMC: 2024 Mar 5.
Published in final edited form as: Eur J Med Chem. 2022 Dec 30;249:115043. doi: 10.1016/j.ejmech.2022.115043

Table 9.

Inhibition of compound 67, 68, 75, and 79 on other P. falciparum kinases

% Activity remaining at 1 μM (IC50)a % control at 1 μMb
PfARK1 PfARK3 PfCDPK2 PfCDPK5 PfGSK3 PfNEK1 PfNEK3 PfPK5 PfPK6 PfPK9 PfPKB PfCDPK1 PfPK5
67 97 100 88 91 97 100 82 97 2 (13 nM) 99 30 51 84
68 98 100 96 98 100 100 84 100 1 (29 nM) 100 38 n.d. n.d.
75 94 97 78 25 30 100 6 94 0 (1.9 nM)c 79 20 n.d. n.d.
79 100 87 64 27 34 100 7 94 1 (1.6 nM)c 89 21 1.1 80
a

Results presented as mean values from experiments using the KinaseSeeker assay performed in duplicate. Variability between individual values is less than 10%. IC50 values were determined using the KinaseSeeker assay with 5-fold dilutions, presented as mean values of two experiments performed in duplicate.

b

Results from DiscoverX KINOMEscan® profiling service.

c

IC50 values approach the kinase concentration in the assay. IC50s < 5 nM treated as equipotent. n.d. = not determined.