Skip to main content
. Author manuscript; available in PMC: 2018 Nov 22.
Published in final edited form as: J Med Chem. 2017 Nov 9;60(22):9184–9204. doi: 10.1021/acs.jmedchem.7b00941

Table 4.

Selectivity against LDHB and other dehydrogenases.a

Analog LDHA
IC50 (μM)		 LDHB
IC50 (μM)		 MDH
IC50 (μM)		 IDH1wt
IC50 (μM)
1 1.34 9.20 >57 >57
2 0.038 1.15 37.8 >57
3 0.424 0.441 >57 >57
33 0.672 0.724 >57 >57
36 2.37 1.51 37.8b >57
37 0.349 0.424 >57 47.4b
38 0.754 0.911 33.7 >57
42 0.095 0.129 >57 >57
43 0.177 0.204 >57 >57
44 0.038 0.049 48.6 47.4
46 0.057 0.078 37.8b >57
47 0.091 0.096 >57 >57
54 0.349 0.259 >57 >57
55 6.23 2.82 >57 >57
56 0.065 0.075 26.8b >57
57 0.053 0.062 48.6 33.5b
58 0.019 0.020 37.8 >57
60 0.110 0.119 >57 26.6
61 0.027 0.020 42.4 33.5
62 0.009 0.008 >57 47.4
63 0.032 0.027 37.8b 29.8
a

IC50 values represent the half maximal (50%) inhibitory concentration as determined in the HTS assay (n = 3).

b

Max. response was less than 50% and thus IC50 values should be considered as lower confidence.