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. Author manuscript; available in PMC: 2016 Dec 14.

Published in final edited form as: Nat Chem Biol. 2015 Oct 5;11(11):878–886. doi: 10.1038/nchembio.1930

Table 1.

Biochemical and cellular IC₅₀ data in nM for GSK321 and GSK990.

GSK321 (Active inhibitor)
IDH1 IC50 (nM)
R132H	R132C	R132G	WT	HT1080 cell 2-HG
4.6^a	3.8^a	2.9^a	46	85
IDH2 IC50 (nM)
R140Q	R172S	WT	R172 U87MG	SW1353 cell 2-HG
1358	1034	496	7940	4689
GSK990 (Inactive inhibitor)
IDH1 IC50 (nM)
R132H	R132C	R132G	WT	HT1080 cell 2-HG
10915	4495	23255	>100000	>36000
IDH2 IC50 (nM)
R140Q	R172S	WT	R172 U87MG	SW1353 cell 2-HG
>100000	>100000	>100000	ND	ND

^a

Determined using tight binding equation as described in methods

ND, Not determined due to lack of biochemical inhibition