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Found 11 Enz. Inhib. hit(s) for PDB: 6B0Z
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  11nMpH: 7.4 T: 2°CAssay Description:The biochemical reactions were performed at room temperature in 384-well Greiner flat-bottom plates (Costar, Cat. No. 781201) using a final reaction ...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  11nMpH: 7.4 T: 2°CAssay Description:Mutant IDH1 R132H catalytic activity was monitored using the quantitative liquid chromatography/mass spectrometry (LC-MS) detection of 2-HG, a produc...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  18nMAssay Description:Inhibition of IDH1 R132H mutant (unknown origin) using alpha-ketoglutarate as substrate by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  20nMAssay Description:Effect on human Glucocorticoid receptor (GR) in a whole cell assay to measure functional cellular GR-antagonism (GRAF)More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  24nMpH: 7.5 T: 2°CAssay Description:The IDH1 (R132H) mutant catalyzes the reduced form of NADP+ (NADPH) and α-ketoglutarate (α-KG) to form nicotinamide adenine dinucleotide ph...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  24nMAssay Description:Inhibition of IDH1 R132H mutant in human HCT116 cells assessed as reduction in 2-HG level after 48 hrs by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  25.5nMpH: 7.5 T: 2°CAssay Description:The IDH1 (R132H) mutant catalyzes the reduced form of NADP+ (NADPH) and α-ketoglutarate (α-KG) to form nicotinamide adenine dinucleotide ph...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  26nMpH: 7.5 T: 2°CAssay Description:The IDH1 (R132H) mutant catalyzes the reduced form of NADP+(NADPH) and α-ketoglutarate (α-KG) to form nicotinamide adenine dinucleotide pho...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  27nMAssay Description:Inhibition of IDH1 R132H mutant (unknown origin) assessed as NADPH consumption using alpha-ketoglutarate as substrate by fluorescence assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  28nMAssay Description:Inhibition of IDH1 R132C mutant (unknown origin) assessed as NADPH consumption using alpha-ketoglutarate as substrate by fluorescence assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM247859(US10112931, Example 466 | US9434719, 466 | US96886...)
Affinity DataIC50:  6.14E+3nMAssay Description:Inhibition of wild-type IDH1 (unknown origin) assessed as NADPH production using isocitrate as substrate by fluorescence assayMore data for this Ligand-Target Pair