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Literature summary for 2.4.2.12 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
Search for more literature for 2.4.2.12

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P43490
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-2780 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Nampt
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
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
0.0000022
-
 pH and temperature not specified in the publication Homo sapiens N-[[4-(benzenesulfonyl)phenyl]methyl]-N''-cyano-N'-pyridin-3-ylguanidine
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
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
0.0000025
-
 pH and temperature not specified in the publication Homo sapiens 2-cyano-1-[4-(phenylsulfonyl)benzyl]-3-pyridin-4-ylguanidine
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
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
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
0.0000054
-
 pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(cyclohexanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
0.0000075
-
 pH and temperature not specified in the publication Homo sapiens N''-cyano-N-[[4-(phenylmethanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
0.000029
-
 pH and temperature not specified in the publication Homo sapiens N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide