BDBM146127 US8957068, 162

SMILES CC(C)[C@H]1COC(=O)N1c1ccnc(N[C@@H](C)c2ccc(Oc3ccccc3)cc2)n1

InChI Key InChIKey=HWEHCJGTUOBELY-UHFFFAOYSA-N

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 146127   

TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Novartis

US Patent
LigandPNGBDBM146127(US8957068, 162)
Affinity DataIC50: 22nMpH: 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
In Depth
Date in BDB:
7/9/2015
Entry Details
Go to US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Novartis

US Patent
LigandPNGBDBM146127(US8957068, 162)
Affinity DataIC50: 31.5nMpH: 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
In Depth
Date in BDB:
7/9/2015
Entry Details
Go to US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Novartis

US Patent
LigandPNGBDBM146127(US8957068, 162)
Affinity DataIC50: 17nMAssay Description: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 Gl...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Novartis

US Patent
LigandPNGBDBM146127(US8957068, 162)
Affinity DataIC50: 1.03E+3nMAssay Description:Inhibition of wild type human IDH1 measured after 2 hrs in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Novartis

US Patent
LigandPNGBDBM146127(US8957068, 162)
Affinity DataIC50: 22nMAssay Description: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 anal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Novartis

US Patent
LigandPNGBDBM146127(US8957068, 162)
Affinity DataIC50: 10nMAssay Description:Inhibition of human N-terminal 6His-tagged IDH1 R132H mutant expressed in Escherichia coli Rosetta2 (DE3) assessed as effect on intracellular 2-HG le...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed