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Literature summary for 2.4.2.12 extracted from

  • Travelli, C.; Aprile, S.; Rahimian, R.; Grolla, A.A.; Rogati, F.; Bertolotti, M.; Malagnino, F.; di Paola, R.; Impellizzeri, D.; Fusco, R.; Mercalli, V.; Massarotti, A.; Stortini, G.; Terrazzino, S.; Del Grosso, E.; Fakhfouri, G.; Troiani, M.P.; Alisi, M.A.; Grosa, G.; Sorba, G.; Canonico, P.L.; Orsomando, G.
    Identification of novel triazole-based nicotinamide phosphoribosyltransferase (NAMPT) inhibitors endowed with antiproliferative and antiinflammatory activity (2017), J. Med. Chem., 60, 1768-1792 .
    View publication on PubMed
Search for more literature for 2.4.2.12

Inhibitors

Inhibitors Comment Organism Structure
(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 Mus musculus
(2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide FK866, potent inhibitor Mus musculus
1-([1,1'-biphenyl]-2-yl)-3-(7-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)heptyl)urea
-
 Mus musculus
3-(1-(4-(2-([1,1'-biphenyl]-2-yloxy)ethyl)benzyl)-1H-1,2,3-triazol-4-yl)pyridine
-
 Mus musculus
3-(1-(6-([1,1'-biphenyl]-2-yloxy)hexyl)-1H-1,2,3-triazol-4-yl)-pyridine
-
 Mus musculus
3-(1-(7-(4-([1,1'-biphenyl]-2-yl)-1H-1,2,3-triazol-1-yl)-heptyl)-1H-1,2,3-triazol-4-yl)pyridine
-
 Mus musculus
3-(1-(7-([1,1'-biphenyl]-2-yloxy)heptyl)-1H-1,2,3-triazol-4-yl)pyridine
-
 Mus musculus
3-(1-(8-([1,1'-biphenyl]-2-yloxy)octyl)-1H-1,2,3-triazol-4-yl)-pyridine
-
 Mus musculus
N-(7-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)heptyl)-[1,1'-biphenyl]-2-carboxamide
-
 Mus musculus
N-(8-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)octyl)biphenyl-2-sulfonamide
-
 Mus musculus
N-([1,1'-biphenyl]-2-yl)-8-(2-(pyridin-3-yl)thiazol-5-yl)-octanamide
-
 Mus musculus
N-([1,1'-biphenyl]-2-yl)-8-(5-(pyridin-3-yl)-1,3,4-oxadiazol-2-yl)octanamide
-
 Mus musculus
N-([1,1'-biphenyl]-2-yl)-8-(5-(pyridin-3-yl)-1H-pyrazol-3-yl)-octanamide
-
 Mus musculus
N-([1,1'-biphenyl]-2-yl)-8-(5-(pyridin-3-yl)-4H-1,2,4-triazol-3-yl)octanamide
-
 Mus musculus
N-([1,1'-biphenyl]-2-yl)-8-(5-(pyridin-3-yl)isoxazol-3-yl)-octanamide
-
 Mus musculus
N-([1,1'-biphenyl]-2-yl)-8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octanamide GPP78 Mus musculus
N-[6-(4-chlorophenoxy)hexyl]-N''-cyano-N'-phenylguanidine CHS828, potent inhibitor Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
nicotinamide D-ribonucleotide + diphosphate Mus musculus
-
 nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Mus musculus Q99KQ4
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
nicotinamide D-ribonucleotide + diphosphate
-
 Mus musculus nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
Nampt
-
 Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000031
-
 at pH 7.5 and 37°C Mus musculus N-(7-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)heptyl)-[1,1'-biphenyl]-2-carboxamide
0.0000038
-
 at pH 7.5 and 37°C Mus musculus 3-(1-(6-([1,1'-biphenyl]-2-yloxy)hexyl)-1H-1,2,3-triazol-4-yl)-pyridine
0.0000049
-
 at pH 7.5 and 37°C Mus musculus (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide
0.0000081
-
 at pH 7.5 and 37°C Mus musculus 3-(1-(7-(4-([1,1'-biphenyl]-2-yl)-1H-1,2,3-triazol-1-yl)-heptyl)-1H-1,2,3-triazol-4-yl)pyridine
0.0000102
-
 at pH 7.5 and 37°C Mus musculus N-([1,1'-biphenyl]-2-yl)-8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octanamide
0.0000156
-
 at pH 7.5 and 37°C Mus musculus 3-(1-(4-(2-([1,1'-biphenyl]-2-yloxy)ethyl)benzyl)-1H-1,2,3-triazol-4-yl)pyridine
0.0000254
-
 at pH 7.5 and 37°C Mus musculus 3-(1-(8-([1,1'-biphenyl]-2-yloxy)octyl)-1H-1,2,3-triazol-4-yl)-pyridine
0.0000313
-
 at pH 7.5 and 37°C Mus musculus 3-(1-(7-([1,1'-biphenyl]-2-yloxy)heptyl)-1H-1,2,3-triazol-4-yl)pyridine
0.0000324
-
 at pH 7.5 and 37°C Mus musculus 1-([1,1'-biphenyl]-2-yl)-3-(7-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)heptyl)urea
0.000047
-
 at pH 7.5 and 37°C Mus musculus N-(8-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)octyl)biphenyl-2-sulfonamide
0.0000499
-
 at pH 7.5 and 37°C Mus musculus N-([1,1'-biphenyl]-2-yl)-8-(5-(pyridin-3-yl)isoxazol-3-yl)-octanamide
0.000269
-
 at pH 7.5 and 37°C Mus musculus N-([1,1'-biphenyl]-2-yl)-8-(5-(pyridin-3-yl)-4H-1,2,4-triazol-3-yl)octanamide