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Inhibition of human recombinant PNMT using AdoMet and DL-norepinephrine hydrocloride as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence based analysis relative to control
Assay data:2 Tested
Summary
Radiochemical Assay for PNMT Activity from Article 10.1021/jm0205752: "Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase."
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Radiochemical Assay of PNMT Inhibitors from Article 10.1021/jm060466d: "Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase."
Assay data:21 Active, 10 Activity ≤ 1 µM, 27 Tested
Primary Screen for Target Class Profiling of Small Molecule Inhibitors of Methyltransferases
Assay data:968 Active, 24930 Tested
Confirmatory Screen for Target Class Profiling of Small Molecule Inhibitors of Methyltransferases
Assay data:902 Active, 1111 Tested
Non-competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli assessed as intercept inhibition constant in presence of 5 uM PEA as substrate and AdoMet as co-substrate by Sigma-plot analysis
Assay data:14 Active, 13 Activity ≤ 1 µM, 21 Tested
Non-competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli assessed as slope inhibition constant in presence of 5 uM PEA as substrate and AdoMet as co-substrate by Sigma-plot analysis
Assay data:17 Active, 14 Activity ≤ 1 µM, 21 Tested
Competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli assessed as inhibition constant using PEA as substrate in presence of 100 uM AdoMet as co-substrate by Sigma-plot analysis
Assay data:16 Active, 14 Activity ≤ 1 µM, 21 Tested
Inhibition of human PNMT expressed in Escherichia coli at 1 uM assessed as reduction in SAH level using DL-normetanephrine as substrate in presence of SAM incubated for 45 mins by LC-MS/MS analysis relative to control
Assay data:1 Tested
Inhibition of human PNMT expressed in Escherichia coli at 10 uM assessed as reduction in SAH level using DL-normetanephrine as substrate in presence of SAM incubated for 45 mins by LC-MS/MS analysis relative to control
Inhibition of human N-terminal His6 tagged PNMT using norepinephrine as substrate preincubated for 10 mins in presence of AdoMet followed by substrate addition by fluorescence based SAHH enzyme coupled assay
Inhibition of human N-terminal His6 tagged PNMT assessed as enzyme activity at 100 uM using norepinephrine as substrate preincubated for 10 mins in presence of AdoMet followed by substrate addition by fluorescence based SAHH enzyme coupled assay relative to control
Inhibition of human N-terminal His6 tagged PNMT assessed as enzyme activity at 33 uM using norepinephrine as substrate preincubated for 10 mins in presence of AdoMet followed by substrate addition by fluorescence based SAHH enzyme coupled assay relative to control
Inhibition of human N-terminal His6 tagged PNMT assessed as enzyme activity at 11 uM using norepinephrine as substrate preincubated for 10 mins in presence of AdoMet followed by substrate addition by fluorescence based SAHH enzyme coupled assay relative to control
Inhibition of human N-terminal His6 tagged PNMT assessed as enzyme activity at 3.7 uM using norepinephrine as substrate preincubated for 10 mins in presence of AdoMet followed by substrate addition by fluorescence based SAHH enzyme coupled assay relative to control
Human Phenylethanolamine N-methyltransferase (Catecholamine turnover)
Assay data:1 Active, 1 Tested
Activity at PNMT in bovine adrenal medulla using DL-beta-phenylethanolamine and SAM-14CH3 as substrate measured per mg of protein by Michaelis-Menten analysis
Assay data:8 Tested
Activity at PNMT in bovine adrenal medulla using DL-beta-phenylethanolamine and SAM-14CH3 as substrate by Michaelis-Menten analysis
Inhibition of bovine adrenal medulla phenylethanolamine N-methyltransferase using 24 to 210 uM S-adenosylmethionine substrate
Assay data:1 Active, 2 Tested
Inhibition of bovine adrenal medulla PNMT at 1 mM by radiochemical technique
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