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Fluorescence Intensity Assay (500 NAD) from US Patent US11304929: "Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors"
Assay data:57 Active, 51 Activity ≤ 1 µM, 57 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Fluorescence Intensity Assay (250 NAD) from US Patent US11304929: "Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors"
Assay data:170 Active, 113 Activity ≤ 1 µM, 191 Tested
Inhibition of N-terminal HIS-tagged and TEV cleavage site containing full length PHGDH (unknown origin) expressed in Escherichia coli assessed as reduction in conversion of 3-Phosphoglycerate and NAD to 3-Phosphohydroxypyruvate and NADH using 250 uM NAD and 500 uM 3-PG incubated for 240 mins by fluorescence based assay
Assay data:171 Active, 114 Activity ≤ 1 µM, 192 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of N-terminal HIS-tagged and TEV cleavage site containing full length PHGDH (unknown origin) expressed in Escherichia coli assessed as reduction in conversion of 3-Phosphoglycerate and NAD to 3-Phosphohydroxypyruvate and NADH using 500 uM NAD and 500 uM 3-PG incubated for 240 mins by fluorescence based assay
Inhibition of PHGDH in human MDA-MB-468 cells assessed as reduction in [13C3]-serine production incubated for 180 mins by LC/MS/MS analysis
Assay data:70 Active, 2 Activity ≤ 1 nM, 57 Activity ≤ 1 µM, 73 Tested
Binding affinity to 3-hydroxyisobutyrate dehydrogenase in human MDA-MB-468 cells at 10 uM incubated for 2 hrs in presence of 12-amino-2-[4-[(1S)-1-[(4,5-dichloro-1,6-dimethyl-indole-2-carbonyl)amino]-2-hydroxy-ethyl]phenyl]sulfonyl-dodecanoic acid by quantitative chemical proteomics assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to Alcohol dehydrogenase class-3 in human MDA-MB-468 cells at 10 uM incubated for 2 hrs in presence of 12-amino-2-[4-[(1S)-1-[(4,5-dichloro-1,6-dimethyl-indole-2-carbonyl)amino]-2-hydroxy-ethyl]phenyl]sulfonyl-dodecanoic acid by quantitative chemical proteomics assay
Inhibition of PHGDH in human MDA-MB-468 cells assessed as reduction in [13C]-serine incubated for 72 hrs using [13C]glucose as substrate by LC-MS/MS analysis
Assay data:2 Active, 2 Tested
Binding affinity to 3-hydroxyisobutyrate dehydrogenase in human MDA-MB-468 cells at 10 uM incubated for 2 hrs in presence of 2-[4-[(1S)-1-[[6-(10-aminodecyl)-4,5-dichloro-1-methyl-indole-2-carbonyl]amino]-2-hydroxy-ethyl]phenyl]sulfonylacetic acid by quantitative chemical proteomics assay
Binding affinity to Alcohol dehydrogenase class-3 in human MDA-MB-468 cells at 10 uM incubated for 2 hrs in presence of 2-[4-[(1S)-1-[[6-(10-aminodecyl)-4,5-dichloro-1-methyl-indole-2-carbonyl]amino]-2-hydroxy-ethyl]phenyl]sulfonylacetic acid by quantitative chemical proteomics assay
Inhibition of N-terminal His6-tagged human PHGDH (4 to 315 residues) assessed as effect on NADH fluorescence incubated for 2 hrs using 3-PG substrate in presence of 250 uM NAD+ and PSAT1 by diaphorase based luminescence assay
Assay data:16 Active, 13 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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