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Literature summary extracted from

  • Travelli, C.; Aprile, S.; Mattoteia, D.; Colombo, G.; Clemente, N.; Scanziani, E.; Terrazzino, S.; Alisi, M.A.; Polenzani, L.; Grosa, G.; Genazzani, A.A.; Tron, G.C.; Galli, U.
    Identification of potent triazolylpyridine nicotinamide phosphoribosyltransferase (NAMPT) inhibitors bearing a 1,2,3-triazole tail group (2019), Eur. J. Med. Chem., 181, 111576 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.12 (2E)-3-(6-aminopyridin-3-yl)-N-((5-[4-(4,4-difluoropiperidine-1-carbonyl)phenyl]-7-(4-fluorophenyl)-1-benzofuran-2-yl)methyl)prop-2-enamide KPT-9274 Homo sapiens
2.4.2.12 (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide FK866 Homo sapiens
2.4.2.12 2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-2-carboxylic acid
-
 Homo sapiens
2.4.2.12 2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
2.4.2.12 2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-4-carboxylic acid
-
 Homo sapiens
2.4.2.12 2'-[(aminooxy)carbonyl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
-
 Homo sapiens
2.4.2.12 2-(4-[[4-(1-ethoxyethenyl)piperidin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-(4-[[4-(propan-2-yl)piperazin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-(4-[[bis(2-hydroxyethyl)amino]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-(pyridin-3-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-[4-[(4-hydroxypiperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-[4-[(4-methylpiperazin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide inhibitor of the extracellular enzyme form Homo sapiens
2.4.2.12 2-[4-[(dimethylamino)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-[4-[(morpholin-4-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 2-[4-[(piperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
 Homo sapiens
2.4.2.12 N-(7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl)[1,1'-biphenyl]-2-carboxamide MV78 Homo sapiens
2.4.2.12 N-([1,1'-biphenyl]-2-yl)-8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octanamide GPP78 Homo sapiens
2.4.2.12 N-[6-(4-chlorophenoxy)hexyl]-N''-cyano-N'-phenylguanidine CHS828 Homo sapiens
2.4.2.12 N-[7-[4-(1-oxo-1lambda(5)-pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
-
 Homo sapiens
2.4.2.12 N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-1-yl)benzamide inhibitor of the intracellular enzyme form Homo sapiens
2.4.2.12 N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-4-yl)benzamide
-
 Homo sapiens
2.4.2.12 N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-[4-[(pyrrolidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]benzamide
-
 Homo sapiens
2.4.2.12 teglarinad water soluble pro-drug of N-[6-(4-chlorophenoxy)hexyl]-N''-cyano-N'-phenylguanidine (CHS828) Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.12 nicotinamide D-ribonucleotide + diphosphate Homo sapiens
-
 nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.12 Homo sapiens P43490
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.12 SH-SY5Y cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.12 nicotinamide D-ribonucleotide + diphosphate
-
 Homo sapiens nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.2.12 Nampt
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.12 0.0000027
-
 pH and temperature not specified in the publication Homo sapiens (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide
2.4.2.12 0.0000031
-
 pH and temperature not specified in the publication Homo sapiens N-(7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl)[1,1'-biphenyl]-2-carboxamide
2.4.2.12 0.0000034
-
 pH and temperature not specified in the publication Homo sapiens N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-1-yl)benzamide
2.4.2.12 0.0000136
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-[(4-methylpiperazin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000171
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-[(piperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000206
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-[[4-(1-ethoxyethenyl)piperidin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000247
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-[[4-(propan-2-yl)piperazin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000254
-
 pH and temperature not specified in the publication Homo sapiens N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-[4-[(pyrrolidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]benzamide
2.4.2.12 0.0000285
-
 pH and temperature not specified in the publication Homo sapiens 2-(pyridin-3-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000385
-
 pH and temperature not specified in the publication Homo sapiens 2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-2-carboxylic acid
2.4.2.12 0.0000418
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-[(4-hydroxypiperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000424
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-[(dimethylamino)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000425
-
 pH and temperature not specified in the publication Homo sapiens N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-4-yl)benzamide
2.4.2.12 0.0000496
-
 pH and temperature not specified in the publication Homo sapiens 2-[4-[(morpholin-4-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000738
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-[[bis(2-hydroxyethyl)amino]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
2.4.2.12 0.0000879
-
 pH and temperature not specified in the publication Homo sapiens 2'-[(aminooxy)carbonyl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
2.4.2.12 0.0005
-
 IC50 above 0.0005 mM, pH and temperature not specified in the publication Homo sapiens 2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-3-carboxylic acid
2.4.2.12 0.0005
-
 IC50 above 0.0005 mM, pH and temperature not specified in the publication Homo sapiens 2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-4-carboxylic acid
2.4.2.12 0.0005
-
 IC50 above 0.0005 mM, pH and temperature not specified in the publication Homo sapiens N-[7-[4-(1-oxo-1lambda(5)-pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide