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Literature summary for 2.4.2.12 extracted from

  • Zheng, X.; Bauer, P.; 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.; Gunzner-Toste, J.; Liederer, B.M.; Ly, J.; OBrien, T.; Oh, A.; Wang, L.; Wang, W.; Xiao, Y.; Zak, M.; Zhao, G.; Yue, Y.u.e.n.
    Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors (2013), J. Med. Chem., 56, 6413-6433.
    View publication on PubMed
Search for more literature for 2.4.2.12

Inhibitors

Inhibitors Comment Organism Structure
1,1-dioxo-N-[[4-[(4-pyrrolidin-1-yl-1-piperidyl)sulfonyl]-phenyl]methyl]-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
 Homo sapiens
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
-
 Homo sapiens
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
-
 Homo sapiens
FK866 i.e. (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide Homo sapiens
GMX-1778 i.e. (E)-1-(6-(4-chlorophenoxy)hexyl)-2-cyano-3-(pyridin-4-yl)-guanidine Homo sapiens
N-(4-[[4-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
 Homo sapiens
N-(pyridin-4-yl)cyclopropanecarboxamide
-
 Homo sapiens
N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]imidazo[1,2-a]pyridine-6-carboxamide
-
 Homo sapiens
N-[4-[(6-methylpyridin-3-yl)sulfonyl]benzyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
 Homo sapiens
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
 Homo sapiens
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
-
 Homo sapiens
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
-
 Homo sapiens
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide potent inhibitor Homo sapiens
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
 Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
 Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
 Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
 Homo sapiens
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
 Homo sapiens
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
 Homo sapiens
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
 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
-
HCT-116 cell
-
 Homo sapiens
-
HT-1080 cell
-
 Homo sapiens
-
MiaPaCa-2 cell
-
 Homo sapiens
-
PC-3 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
PBEF
-
 Homo sapiens
pre-B-cell colony-enhancing factor
-
 Homo sapiens
Visfatin
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000011
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.000002
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.000003
-
 pH and temperature not specified in the publication Homo sapiens 1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
0.0000038
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000044
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000047
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
0.000005
-
 pH and temperature not specified in the publication Homo sapiens trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000051
-
 pH and temperature not specified in the publication Homo sapiens trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000066
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
0.0000072
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000076
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
0.0000078
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
0.0000088
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.000009
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0000095
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
0.00001
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
0.00001
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
0.000012
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.000012
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.000021
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
0.000036
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
0.000049
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
0.000062
-
 pH and temperature not specified in the publication Homo sapiens 1,1-dioxo-N-[[4-[(4-pyrrolidin-1-yl-1-piperidyl)sulfonyl]-phenyl]methyl]-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
0.000063
-
 pH and temperature not specified in the publication Homo sapiens N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
0.00046
-
 pH and temperature not specified in the publication Homo sapiens trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
0.0013
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
0.0015
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
0.0016
-
 pH and temperature not specified in the publication Homo sapiens trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
0.002
-
 pH and temperature not specified in the publication Homo sapiens N-(pyridin-4-yl)cyclopropanecarboxamide
0.002
-
 pH and temperature not specified in the publication Homo sapiens trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
0.002
-
 pH and temperature not specified in the publication Homo sapiens trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
0.002
-
 pH and temperature not specified in the publication Homo sapiens tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
0.002
-
 pH and temperature not specified in the publication Homo sapiens tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
0.23
-
 pH and temperature not specified in the publication Homo sapiens 7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide