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Inhibition of human N-terminal 6His-tagged IDH1 R132C mutant expressed in Escherichia coli Rosetta2 (DE3) measured after 45 mins in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human wild type IDH1/IDH1 R132H mutant heterodimer in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of wild type human IDH1 upto 50 uM measured after 2 hrs in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human N-terminal 6His-tagged IDH1 R132H mutant expressed in Escherichia coli Rosetta2 (DE3) assessed as effect on intracellular 2-HG level incubated for 60 mins in presence of alpha-ketoglutarate and NADPH by LC/MS/MS analysis
Assay data:25 Active, 21 Activity ≤ 1 µM, 26 Tested
Inhibition of IDH1 R132H mutant expressed in human HCT-116 cells assessed as effect on intracellular 2-HG level incubated for 48 hrs by LC/MS/MS analysis
Assay data:21 Active, 16 Activity ≤ 1 µM, 21 Tested
Inhibition of wild type human IDH1 measured after 2 hrs in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of IDH1 R132H mutant expressed in human MCF-10A cells assessed as effect on intracellular 2-HG level incubated for 5 days by Cell Titer Glo assay
In vivo inhibition of IDH1 R132H mutant in po dosed athymic nu/nu mouse xenografted with human HCT-116 cells assessed as effect on 2-HG level in tumor upto 600 mg/kg
In vivo inhibition of IDH1 R132H mutant in po dosed athymic nu/nu mouse xenografted with human HCT-116 cells assessed as inhibition of 2-HG production in tumor at 200 mg/kg measured upto 36 hrs
Assay data:1 Active, 1 Tested
In vivo inhibition of IDH1 R132H mutant in po dosed athymic nu/nu mouse xenografted with human HCT-116 cells assessed as elimination of 2-HG in tumor tissue at 200 mg/kg measured upto 36 hrs
In vivo inhibition of IDH1 R132H mutant in po dosed athymic nu/nu mouse xenografted with human HCT-116 cells assessed as inhibition of 2-HG production in tumor at 200 mg/kg measured after 8 to 12 hrs
In vivo inhibition of IDH1 R132H mutant in athymic nu/nu mouse xenografted with human HCT-116 cells assessed as elimination of 2-HG in tumor tissue at 25 mg/kg, po bid administered twice every 12 hrs measured after 48 hrs
In vivo inhibition of IDH1 R132H mutant in athymic nu/nu mouse xenografted with human HCT-116 cells assessed as elimination of 2-HG in tumor tissue at 25 mg/kg, po bid administered twice every 12 hrs measured after 24 hrs
Inhibition of human N-terminal 6His-tagged IDH1 R132H mutant expressed in Escherichia coli Rosetta2 (DE3) measured after 90 mins in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
In vivo inhibition of IDH1 R132H mutant in athymic nu/nu mouse xenografted with human HCT-116 cells assessed as effect on DNA methylation in tumor at 25 mg/kg, po bid administered twice every 12 hrs measured after 24 hrs
Inhibition of IDH1 R132H mutant (unknown origin)
Assay data:1 Active, 2 Tested
Binding affinity to human IDH1 assessed as binding constant (Kon) in presence of NADPH and alpha-ketoglutarate by spectrophotometry analysis
Binding affinity to human IDH1 assessed as binding constant (Koff) in presence of NADPH and alpha-ketoglutarate by spectrophotometry analysis
In Vitro Assay for IDH1m (R132H or R132C) Inhibitors from US Patent US11667673: "Therapeutically active compounds and their methods of use"
Assay data:190 Active, 189 Activity ≤ 1 µM, 190 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Biochemical Assays for IDH1 and IDH2 Mutant Enzymes from US Patent US11649247: "7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors"
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
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