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. 2018 Sep 12;61(18):8374–8389. doi: 10.1021/acs.jmedchem.8b00884

Table 5. DMPK Data for Selected Compounds.

cmpd TbNMT IC50 (nM) HsNMT IC50 (nM) T. brucei EC50 (nM) enzyme selectivity S Cli mouse microsomes mL–1 min–1 g–1 mouse brain:blood ratio mouse PPB (fu) hERGa IC50/μM
Quinoline Series
32 <5 250 19 >50 13 6.2      
34 <5 640 40 >130 16 6.2 0.8 0.17 1.3
37 6 1400 59 59 24 1.8 0.8 0.093  
41 7 27000 91 3900 300 1.5 0.8 0.18 1.6
Indazole Series
54 <5 230 5 >46 46 2.9 <0.1 0.062 3.7
58 <5 2500 31 >500 80 3.7 <0.1   3.0
60 5 12000 39 2500 320 1.4 <0.1   3.3
62 7 4600 220 660 21 20     3.1
63 <5 190 26 >38 7 24     5.6
64 <5 130 9 >26 14 22     6.7
a

hERG values were determined using IonWorks patch-clamp electrophysiology at Essen Bioscience, UK.