. Author manuscript; available in PMC: 2018 Dec 1.

Published in final edited form as: Eur J Med Chem. 2017 Oct 6;141:446–459. doi: 10.1016/j.ejmech.2017.10.007

Table 2.

Biological assay results of the linker replacement library.


Entry	R	LogP	MPO Score	T. brucei EC₅₀ (μM)^a	T. brucei LLE
2^b		7.3	2.8	0.042	0.1
17 NEU-1008		6.5	1.8	1.4	-0.6
18 NEU-1011		6.5	1.8	0.41	-0.1
21 NEU-1009		4.7	1.7	3.1	0.8
23 NEU-2083		5.1	1.8	0.61	1.1
26 NEU-2078		5.3	1.1	0.78	0.8

Compounds showing >75% growth inhibition at 5 μM for T.b. brucei were tested for EC₅₀ values. T.b. brucei EC₅₀ values are the result of duplicate experiments, within ± 24%.

Previously reported data.[12]