Table 2. SAR at position 4.

ID	R4	R2	Pf3D7 IC50 (nM)*	G9a IC50 (nM)*	G9a/Pf3D7	HepG2 IC50 (nM)	HepG2/Pf3D7	clog P	TPSA
18			74	116	1.6	3100	41.9	3.78	65.99
19			69	78	1.1	3300	47.8	3.78	65.99
20			80	169	2.1	4100	51.2	3.78	65.99
21			NT	112	—	ND	ND	3.61	65.99
22			148	132	0.9	ND	ND	3.61	65.99
23			137	116	0.8	ND	ND	3.61	65.99
24			237	128	0.5	ND	ND	3.48	75.22
25			77	869	11.3	2800	36.4	5.02	62.75
26			77	690	9.0	2700	35.1	5.02	62.75
27			78	∼1000	∼12.8	2900	37.2	5.02	62.75
28			191	1214	6.4	ND	ND	4.85	62.75
29			NT	∼1000	—	ND	ND	4.85	62.75
30			197 a	∼1000	∼5.1	10 500	53.3	3.48	65.99
31			178 a	∼1000	∼5.6	6300	35.4	4.71	62.75
32			330 a	344	1.0	ND	ND	3.09	65.99
33			94 a	830	8.8	6300	67	4.32	62.75
34			93 a	∼10 000	∼107.5	5600	60.2	4.06	78.88
35			247 a	>10 000	>40.5	ND	ND	4.08	95.95
36			369 a	>10 000	>27.1	ND	ND	4.35	79.82
37			107 a	>1000	>9.3	17 800	166.3	3.55	79.82
38			>300 a	330 b /230 c	—	ND	ND	2.30	65.99
39			>300 a	680 b /200 c	—	ND	ND	1.90	65.99
40			37 a	591	16.0	14 200	383.8	3.14	62.75
41			56 a	>1000	>17.9	5500	98.2	2.88	78.88
42			28 a	910 b /6500 c	—	>10 000	>357	3.00	62.75
43			34 a	1100 b /900 c	—	>10 000	>294	2.22	62.75
44			174	10	0.06	ND	ND	4.25	65.99
45			130	25	0.19	ND	ND	3.86	65.99
46			144	295	2.0	ND	ND	5.09	62.75
47			47	185	3.9	ND	ND	4.72	71.98
48			205	55	0.27	ND	ND	4.00	65.99
49			222	49	0.22	ND	ND	3.61	65.99
50			108	NT	—	ND	ND	4.85	62.75
51			470	55	0.12	ND	ND	3.07	65.99
52			280	123	0.44	ND	ND	2.68	65.99
53			126	NT	—	ND	ND	3.55	71.98
54			71	319	4.5	ND	ND	3.92	62.75
55			215	6438	29.9	ND	ND	3.14	62.75
56			107	3877	36.2	ND	ND	3.53	62.75
57			570 a	>10 000	>17.5	ND	ND	3.14	62.75
58			161 a	>10 000	>62.1	ND	ND	4.38	59.51
59			77 a	>10 000	>129.9	12 200	158.4	4.87	59.51

^aParasite-killing activity reported earlier.33

^bIC₅₀ reported using enzyme-coupled SAH detection (ECSD) assay.36,37

^cIC₅₀ reported using chemiluminescence-based oxygen tunnelling (CLOT) assay.36,37