. Author manuscript; available in PMC: 2021 Jan 25.

Published in final edited form as: J Med Chem. 2020 Sep 27;63(19):10984–11011. doi: 10.1021/acs.jmedchem.0c00916

Table 4.

Biochemical and Cellular LDH Inhibition of Compounds 68–73



Compd No.		X	Biochemical LDHA IC₅₀ (nM)^a	A673 cells		MiaPaCa-2 cells		HEK293 Cells
Compd No.		X	Biochemical LDHA IC₅₀ (nM)^a	lactate inh IC₅₀ (nM)^a	Cytotox IC₅₀ (nM)^a	lactate inh IC₅₀ (nM)^a	Cytotox IC₅₀ (nM)^a	CETSA IC₅₀ (nM)^a

68		H	52	357	452	331	471	158
69		F	74	371	488	149	454	108
70		F	15	320	833	231	837	134
71	CH₃	F	11	405	614	321	528	126
72		F	59	361	2263	255	1899	112
73	-	-	39	713	16023	972	17376	398

IC₅₀ values represent the half maximal (50%) inhibitory concentration as determined in the HTS assay using a dose response in the 1536-well format. (n = 2 for lactate and n = 3 for cytotoxicity, CETSA, and biochemical LDHA.)