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Table 1 In vitro inhibition of the inhibitors with homodimeric IDH enzymes

From: Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells

Enzymes assayed

Incubation time (hours)

IC50 (nM)

CP-17

AGI-6780

Enasidenibc

IDH2/R140Qa

1

99.88

16.39

320

16

40.75

12.83

100

IDH2/WTb

16

2267

99.95

1800

Selectivity

16

55.6

7.8

18

IDH1/R132Ha

16

> 5000

  

IDH1/WTb

16

> 5000

  
  1. a IC50 for α-KG reduction; b IC50 for isocitrate to α-KG; c IC50 reported from reference [16]