Compile Data Set for Download or QSAR
Report error Found 7995 Enz. Inhib. hit(s) with BLAST sequence identity > 85%
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247849(US9688672, Example 456 | US9434719, 456 | US101129...)
Affinity DataIC50: 1nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247849(US9688672, Example 456 | US9434719, 456 | US101129...)
Affinity DataIC50: 1nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 1nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM116236(US8637508, 11 | US10035794, Example 11 | US1068328...)
Affinity DataIC50: 2nMAssay Description:Chinese hamster ovary cells are transfected with the human gene for amyloid precursor protein. The cells are plated at a density of 8000 cells/well i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM296116(US10112931, Example 467 | (R)-3-(2-(((S)-1-(5-(2-f...)
Affinity DataIC50: 2.29nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM497343(7-[[(1S)-1-[4-[2- Cyclopropyl-1-(4-prop-2- enoylpi...)
Affinity DataIC50: 2.76nMAssay Description:IDH1-R132H, IDH1-R132C, IDH2-R172K and IDH2-R140Q mutant enzymes catalyze the conversion of αKG to 2HG. 2HG is analyzed using in-line solid phas...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM497343(7-[[(1S)-1-[4-[2- Cyclopropyl-1-(4-prop-2- enoylpi...)
Affinity DataIC50: 2.76nMAssay Description:IDH1-R132H, IDH1-R132C, IDH2-R172K and IDH2-R140Q mutant enzymes catalyze the conversion of αKG to 2HG. 2HG is analyzed using in-line solid phas...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM497343(7-[[(1S)-1-[4-[2- Cyclopropyl-1-(4-prop-2- enoylpi...)
Affinity DataIC50: 2.76nMAssay Description:IDH1-R132H, IDH1-R132C, IDH2-R172K and IDH2-R140Q mutant enzymes catalyze the conversion of αKG to 2HG. 2HG is analyzed using in-line solid phas...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM116247(US8637508, 24 | US10035794, Example 24 | US1068328...)
Affinity DataIC50: 3nMAssay Description:Chinese hamster ovary cells are transfected with the human gene for amyloid precursor protein. The cells are plated at a density of 8000 cells/well i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM116257(US8637508, 34 | US10035794, Example 34 | US1068328...)
Affinity DataIC50: 3nMAssay Description:Chinese hamster ovary cells are transfected with the human gene for amyloid precursor protein. The cells are plated at a density of 8000 cells/well i...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247707(US9688672, Example 309 | US9434719, 309 | US101129...)
Affinity DataIC50: 3nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247707(US9688672, Example 309 | US9434719, 309 | US101129...)
Affinity DataIC50: 3nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247707(US9688672, Example 309 | US9434719, 309 | US101129...)
Affinity DataIC50: 3nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247707(US9688672, Example 309 | US9434719, 309 | US101129...)
Affinity DataIC50: 3nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287785(US10086000, Example 63 | 2-Methyl-2-[6-(6,7,8,9-te...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287795(US10086000, Example 13 | 2-[6-(2,3-dihydro-1H- ind...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287785(US10086000, Example 63 | 2-Methyl-2-[6-(6,7,8,9-te...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287848(US10086000, Example 65 | 8-(1,3-dihydro-2H- isoind...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287883(US10086000, Example 100 | 8-(1,2-dimethyl-1H- imid...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287886(US10086000, Example 103 | 8-isoxazol-4-yl-6-(6,7,8...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287889(US10086000, Example 106 | 1-{4-[6-(6,7,8,9-tetrahy...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287908(US10086000, Example 125 | 4-Methyl-5-[6-(6,7,8,9-t...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287909(US10086000, Example 126 | (4R)-4-(1-Methylethyl)-3...)
Affinity DataIC50: 3nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287908(US10086000, Example 125 | 4-Methyl-5-[6-(6,7,8,9-t...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM416187(6-{[(1S,4S)-4-ethoxy-3,3- difluorocyclohexyl]carbo...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287889(US10086000, Example 106 | 1-{4-[6-(6,7,8,9-tetrahy...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287883(US10086000, Example 100 | 8-(1,2-dimethyl-1H- imid...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287848(US10086000, Example 65 | 8-(1,3-dihydro-2H- isoind...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM416186(6-{[(1R,4R)-4-ethoxy-3,3- difluorocyclohexyl]carbo...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287795(US10086000, Example 13 | 2-[6-(2,3-dihydro-1H- ind...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287886(US10086000, Example 103 | 8-isoxazol-4-yl-6-(6,7,8...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287909(US10086000, Example 126 | (4R)-4-(1-Methylethyl)-3...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM389389(US9951027, 2-155-2)
Affinity DataIC50: 3nMAssay Description:mIDH1 catalyzes the NADPH-dependent reduction of alpha-ketoglutarate (α-KG) to (2R)-2-hydroxyglutarate (2-HG). NADPH consumption was measured by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287785(US10086000, Example 63 | 2-Methyl-2-[6-(6,7,8,9-te...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287785(US10086000, Example 63 | 2-Methyl-2-[6-(6,7,8,9-te...)
Affinity DataIC50: 3nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM412559(US10399972, Example 50)
Affinity DataIC50: 3.5nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand Info
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM412560(US10399972, Example 51 | (3,9-difluoro-8-(1H-pyraz...)
Affinity DataIC50: 3.60nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand Info
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247614(US9688672, Example 216 | US9434719, 216 as TFA sal...)
Affinity DataIC50: 4nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247567(US9688672, Example 133 | US9434719, 133 | US101129...)
Affinity DataIC50: 4nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247614(US9688672, Example 216 | US9434719, 216 as TFA sal...)
Affinity DataIC50: 4nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247707(US9688672, Example 309 | US9434719, 309 | US101129...)
Affinity DataIC50: 4nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM247707(US9688672, Example 309 | US9434719, 309 | US101129...)
Affinity DataIC50: 4nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287847(US10086000, Example 64 | 8-bromo-6-(6,7,8,9- tetra...)
Affinity DataIC50: 4nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287903(US10086000, Example 120 | 4-[6-(6,7,8,9-Tetrahydro...)
Affinity DataIC50: 4nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287907(US10086000, Example 124 | 3-[6-(6,7,8,9-Tetrahydro...)
Affinity DataIC50: 4nMpH: 7.0 T: 2°CAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM389364(US9951027, 2-144-2)
Affinity DataIC50: 4nMAssay Description:mIDH1 catalyzes the NADPH-dependent reduction of alpha-ketoglutarate (α-KG) to (2R)-2-hydroxyglutarate (2-HG). NADPH consumption was measured by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287907(US10086000, Example 124 | 3-[6-(6,7,8,9-Tetrahydro...)
Affinity DataIC50: 4nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM287903(US10086000, Example 120 | 4-[6-(6,7,8,9-Tetrahydro...)
Affinity DataIC50: 4nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM416251(US10442819, Example 395 | 4-(6-{[trans-4-(1- methy...)
Affinity DataIC50: 4nMAssay Description:Each test compound (10 mM stock in DMSO) is diluted in DMSO to make a 10-point, 3-fold dilution series. 125 nL of each dilution or DMSO alone is disp...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H] Isocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Novartis

US Patent
LigandPNGBDBM389324(US9951027, 2-96-2 | US9951027, 2-95-2)
Affinity DataIC50: 4nMAssay Description:mIDH1 catalyzes the NADPH-dependent reduction of alpha-ketoglutarate (α-KG) to (2R)-2-hydroxyglutarate (2-HG). NADPH consumption was measured by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

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