Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Zheng, X.; Baumeister, T.; Buckmelter, A.J.; Caligiuri, M.; Clodfelter, K.H.; Han, B.; Ho, Y.C.; Kley, N.; Lin, J.; Reynolds, D.J.; Sharma, G.; Smith, C.C.; Wang, Z.; Dragovich, P.S.; Oh, A.; Wang, W.; Zak, M.; Wang, Y.; Yuen, P.W.; Bair, K.W.
    Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors (2014), Bioorg. Med. Chem. Lett., 24, 337-343.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.12 1-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)urea
-
Homo sapiens
2.4.2.12 2-cyano-1-[4-(phenylsulfonyl)benzyl]-3-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 APO-866
-
Homo sapiens
2.4.2.12 GMX-1777
-
Homo sapiens
2.4.2.12 GMX-1778
-
Homo sapiens
2.4.2.12 N''-cyano-N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethoxy)benzene-1-sulfonyl]phenyl]methyl)guanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethyl)benzene-1-sulfonyl]phenyl]methyl)guanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-pyridin-4-yl-N'-[[4-(quinoline-8-sulfonyl)phenyl]methyl]guanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(3-methoxybenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-3-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(cyclohexanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(phenylmethanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N''-cyano-N-[[4-(pyridine-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
Homo sapiens
2.4.2.12 N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide
-
Homo sapiens
2.4.2.12 N-[[4-(benzenesulfonyl)phenyl]methyl]-N''-cyano-N'-pyridin-3-ylguanidine
-
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 + 5-phospho-alpha-D-ribose 1-diphosphate Homo sapiens
-
nicotinamide D-ribonucleotide + 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 A-2780 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.12 nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
-
Homo sapiens nicotinamide D-ribonucleotide + 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 0.0000006
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
2.4.2.12 0.0000017
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-N'-pyridin-4-ylguanidine
2.4.2.12 0.0000019
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(3-methoxybenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
2.4.2.12 0.000002
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(pyridine-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
2.4.2.12 0.0000022
-
pH and temperature not specified in the publication Homo sapiens N-[[4-(benzenesulfonyl)phenyl]methyl]-N''-cyano-N'-pyridin-3-ylguanidine
2.4.2.12 0.0000024
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
2.4.2.12 0.0000024
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethyl)benzene-1-sulfonyl]phenyl]methyl)guanidine
2.4.2.12 0.0000025
-
pH and temperature not specified in the publication Homo sapiens 2-cyano-1-[4-(phenylsulfonyl)benzyl]-3-pyridin-4-ylguanidine
2.4.2.12 0.0000036
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-pyridin-4-yl-N'-[[4-(quinoline-8-sulfonyl)phenyl]methyl]guanidine
2.4.2.12 0.0000044
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-3-ylguanidine
2.4.2.12 0.0000044
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethoxy)benzene-1-sulfonyl]phenyl]methyl)guanidine
2.4.2.12 0.0000054
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(cyclohexanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
2.4.2.12 0.0000075
-
pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(phenylmethanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
2.4.2.12 0.000029
-
pH and temperature not specified in the publication Homo sapiens N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide