2.1.1.1: nicotinamide N-methyltransferase
This is an abbreviated version!
For detailed information about nicotinamide N-methyltransferase, go to the full flat file.
Reaction
Synonyms
ANMT-1, B0303.2, methyltransferase, nicotinamide, nicotinamide N-methyl transferase, nicotinamide N-methyltransferase, NNMT
ECTree
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Inhibitors
Inhibitors on EC 2.1.1.1 - nicotinamide N-methyltransferase
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3-(6-amino-6-oxohexyl)benzamide
inhibitor mimics the transition state of the methylation reaction
5'-([(3S)-3-amino-3-carboxypropyl][[3-(methoxycarbonyl)phenyl]methyl]amino)-5'-deoxyadenosine
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5'-deoxy-5'-[[(3S)-3,4-diamino-4-oxobutyl][(naphthalen-2-yl)methyl]amino]adenosine
inhibitor demonstrates a dose-dependent inhibitory effect on the cell proliferation of the HSC-2 human oral cancer cell line
5'-[(3-amino-3-carboxypropyl)[3-(3-carbamoyl-4-methylphenyl)prop-2-yn-1-yl]amino]-5'-deoxyadenosine
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5'-[(3-amino-3-carboxypropyl)[3-(3-carbamoylphenyl)prop-2-yn-1-yl]amino]-5'-deoxyadenosine
compound exhibits around 1000fold selectivity for NNMT over other methyltransferases and almost 100fold selectivity for S-5'-adenosyl-L-homocysteine hydrolase
5'-[(3-amino-3-carboxypropyl)[3-(5-carbamoyl-2-methoxyphenyl)prop-2-yn-1-yl]amino]-5'-deoxyadenosine
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5'-[(4-amino-4-oxobutyl)[(naphthalen-2-yl)methyl]amino]-5'-deoxyadenosine
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5'-[(5-amino-5-oxopentyl)[(naphthalen-2-yl)methyl]amino]-5'-deoxyadenosine
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5'-[[(3S)-3-amino-3-carboxypropyl][(3-carboxyphenyl)methyl]amino]-5'-deoxyadenosine
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5'-[[(3S)-3-amino-3-carboxypropyl][4-(3-carbamoylphenyl)butyl]amino]-5'-deoxyadenosine
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5-[[(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]-7-(3-carbamoylphenyl)hept-6-ynoic acid
log Ki value 4.65
6-(methylamino)pyridine-3-carboxamide
compound inhibits NNMT enzymatic activity and reduces the formation of 1-methyl-nicotinamide by about 80% at 2 h when dosed in mice orally at 50 mg/kg
7-(3-carbamoylphenyl)hept-6-ynoic acid
inhibitor mimics the transition state of the methylation reaction
9-(9-amino-5,6,7,8,9-pentadeoxy-6-ethynyl-beta-D-ribo-decofuranuronosyl)-9H-purin-6-amine
log Ki value 4.32
9-[9-amino-6-[(2-carbamoylphenyl)ethynyl]-5,6,7,8,9-pentadeoxy-beta-D-ribo-decofuranuronosyl]-9H-purin-6-amine
log Ki value 4.71
9-[9-amino-6-[(3-carbamoylphenyl)ethynyl]-5,6,7,8,9-pentadeoxy-beta-D-ribo-decofuranuronosyl]-9H-purin-6-amine
high-affinity, subnanomolar NNMT inhibitor
Nickel
exposure of BEAS-2B cells to induces NNMT repression at both the protein and mRNA levels
additional information
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not inhibitory: Ca2+, SKF 525A, 3,4-dimethoxy-5-hydroxybenzoic acid
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bisubstrate inhibitor, competitive with respect to S-adenosyl-L-methionine, noncompetitive with respect to nicotinamide
5'-[[(3S)-3-amino-3-carboxypropyl][(3-carbamoylphenyl)methyl]amino]-5'-deoxyadenosine
inhibitor mimics the transition state of the methylation reaction
N1-methylnicotinamide
-
IC50 0.06 mM for human protein, 0.03 mM for recombinant protein