. Author manuscript; available in PMC: 2024 Apr 14.

Published in final edited form as: ACS Infect Dis. 2023 Mar 15;9(4):1004–1021. doi: 10.1021/acsinfecdis.3c00025

Table 2.

Antiplasmodial and Kinase Activities of PLK1 Inhibitors


ID	antiplasmodial activity			cytotoxicity		kinase activity
ID	Pf Dd2 EC₅₀ (nM)	Pf 3D7 EC₅₀ (nM)	RI^a	HepG2 EC₅₀ (nM)	SI^b	PLK1 IC₅₀ (nM)
BI-6727 (11)	230 ± 14	284 ± 52	0.81	1930 ± 460	8.0	0.87
GSK461364 (12)	533 ± 78	1410 ± 77	0.34	1910 ± 210	4.0	2.2
MLN0905 (13)	1820 ± 260	nt	-	3940 ± 110	2.0	2.0
SBE 13 (14)	3570 ± 130	nt	-	>25,000	>7.0	0.20
NMS-P937 (15)	>5000	nt	-	6010 ± 79	<1.0	2.0
ON-01910 (16)	>5000	nt	-	11,900 ± 42	<2.0	9.0
GW843682 (17)	>5000	nt	-	>25,000	-	2.2
Compound 18	336 ± 34	315 ± 11	1.1	1870 ± 190	6.0	3.3
Compound 19	971 ± 58	759 ± 96	1.3	2740 ± 310	2.0	4.6
Compound 20	1990 ± 34	1860 ± 330	1.1	4090 ± 440	2.0	4.3
Compound 21	2020 ± 150	2020 ± 340	1	6840 ± 210	3.0	29
Compound 22	2530 ± 130	nt	-	4690 ± 690	2.0	4.9
Compound 23	2780 ± 290	nt	-	4300 ± 450	2.0	<0.50

Resistance Index (RI) = Dd2 EC₅₀/3D7 EC₅₀.

50 Selectivity Index (SI) = HepG2 EC₅₀/Dd2 EC₅₀.

50 nt = not tested.

Values shown are the average EC₅₀ ± SEM from at least three biological replicates. Human PLK1 IC₅₀ values were obtained from prior publication or from Selleck Chemicals.^15,16