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Isothermal Titration Calorimetry (ITC) from US Patent US10513520: "Sulfamide and sulfamate inhibitors of hHint1"
Assay data:5 Active, 3 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of PKCi in human NCI-H929 cells at 10 uM by mass spectroscopic analysis relative to control
Assay data:6 Tested
SummaryRelated BioAssays by Target
Inhibition of PKCi in human NCI-H929 cells by mass spectroscopic analysis
Prodrug activation assessed as human HINT1 mediated compound hydrolysis at 200 nM measured up to 120 mins by UV-RP-HPLC analysis
Assay data:2 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Prodrug activation assessed as human HINT1 mediated compound hydrolysis at 20 nM measured up to 120 mins by UV-RP-HPLC analysis
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of full-length human N-terminal His6-tagged Hint1 expressed in Escherichia coli Rosetta 2 pLysS cells assessed as ratio of Kcat to Km
Binding affinity to full-length human N-terminal His6-tagged Hint1 expressed in Escherichia coli Rosetta 2 pLysS cells by isothermal titration calorimetry
Assay data:10 Active, 3 Activity ≤ 1 µM, 12 Tested
Inhibition of human N-terminal His6-tagged Hint1 expressed in Escherichia coli Rosetta 2 pLysS cells by fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Potency index, ratio of GMP Kd to compound Kd for His-tagged human full length HINT1
Assay data:1 Tested
Binding affinity to recombinant human HINT1 by isothermal titration calorimetric assay
Assay data:1 Active, 1 Tested
Binding affinity to His-tagged human full length HINT1 expressed in Rosetta2 pLysS cells by isothermal titration calorimetric assay
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of His-tagged human full length HINT1 expressed in Rosetta2 pLysS cells using TrpAMP as substrate measured for 2 to 30 mins by fluorescence assay
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of PKCi in human SKCO1 cells at 1 uM after 4 hrs using biotin labeled DLKLDNVLLDSEGHIK probe by mass-spectrometric analysis relative to control
Assay data:3 Tested
Prodrug activation in human GRANTA-519 cells assessed as hint1-mediated 2-amino-7-(2-(4-chlorophenoxy)ethyl)-9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(phosphonooxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-7-ium formation per 5 million cells at 150 uM after 12 hrs by LC-MS/MS analysis relative to 9-((2R,3R,4S,5R)-5-(((((2-(1H-Indol-3-yl)ethyl)amino)-(hydroxy)phosphoryl)oxy)methyl)-3,4-dihydroxytetrahydrofuran-2-yl)-2-amino-7-(2-(4-chlorophenoxy)ethyl)-6-oxo-6,9-dihydro-1H-purin-7-ium
Prodrug activation in human Z138 cells assessed as hint1-mediated 2-amino-7-(2-(4-chlorophenoxy)ethyl)-9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(phosphonooxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-7-ium formation per 5 million cells at 150 uM after 12 hrs by LC-MS/MS analysis relative to 9-((2R,3R,4S,5R)-5-(((((2-(1H-Indol-3-yl)ethyl)amino)-(hydroxy)phosphoryl)oxy)methyl)-3,4-dihydroxytetrahydrofuran-2-yl)-2-amino-7-(2-(4-chlorophenoxy)ethyl)-6-oxo-6,9-dihydro-1H-purin-7-ium
Prodrug activation in human GRANTA-519 cells assessed as Hint1 mediated 2-amino-7-(2-(4-chlorophenoxy)ethyl)-9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(phosphonooxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-7-ium formation per 5 million cells at 150 uM after 12 hrs by LC-MS/MS analysis
Prodrug activation in human Z138 cells assessed as Hint1 mediated 2-amino-7-(2-(4-chlorophenoxy)ethyl)-9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(phosphonooxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-7-ium formation per 5 million cells at 150 uM after 12 hrs by LC-MS/MS analysis
Prodrug activation in human Mino cells assessed as Hint1 mediated 2-amino-7-(2-(4-chlorophenoxy)ethyl)-9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(phosphonooxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-7-ium formation per 5 million cells at 150 uM after 12 hrs by LC-MS/MS analysis
Drug metabolism in human HuH7 cells assessed as HINT1-mediated ((2R,3R,4R,5R)-5-(4-butyramido-2-oxopyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methyl dihydrogen phosphate metabolite formation at 50 uM after 48 hrs by LC/MS/MS analysis
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