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Literature summary extracted from

  • Xu, T.Y.; Zhang, S.L.; Dong, G.Q.; Liu, X.Z.; Wang, X.; Lv, X.Q.; Qian, Q.J.; Zhang, R.Y.; Sheng, C.Q.; Miao, C.Y.
    Discovery and characterization of novel small-molecule inhibitors targeting nicotinamide phosphoribosyltransferase (2015), Sci. Rep., 5, 10043.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.12 (1Z)-N'-(benzoyloxy)-3-(2-oxo-1,3-benzoxazol-3(2H)-yl)propanimidamide
-
 Homo sapiens
2.4.2.12 (2R,2'R)-5,5',7,7'-tetrahydroxy-2,2'-bis(4-hydroxyphenyl)-2,2',3,3'-tetrahydro-4H,4'H-[3,8'-bi-1-benzopyran]-4,4'-dione
-
 Homo sapiens
2.4.2.12 1-(pyridin-3-ylmethyl)-3-[4-(pyrrolidin-1-ylsulfonyl)phenyl]thiourea
-
 Homo sapiens
2.4.2.12 1-[3-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea potent inhibitor Homo sapiens
2.4.2.12 1-[4-(morpholin-4-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
 Homo sapiens
2.4.2.12 1-[4-(piperazin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
 Homo sapiens
2.4.2.12 1-[4-(piperidin-1-ylcarbonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
 Homo sapiens
2.4.2.12 1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)guanidine
-
 Homo sapiens
2.4.2.12 1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)urea
-
 Homo sapiens
2.4.2.12 1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)guanidine
-
 Homo sapiens
2.4.2.12 1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)urea
-
 Homo sapiens
2.4.2.12 1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-4-ylmethyl)thiourea
-
 Homo sapiens
2.4.2.12 1-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
 Homo sapiens
2.4.2.12 4-chloro-N-[(5-[[(6-fluoro-4H-1,3-benzodioxin-8-yl)methyl]sulfamoyl]thiophen-2-yl)methyl]benzamide
-
 Homo sapiens
2.4.2.12 ethyl [(E)-[4-(piperidine-1-sulfonyl)anilino][[(pyridin-3-yl)methyl]amino]methylidene]carbamate
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(1H-benzimidazol-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(2,6-difluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(2-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(2-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(2-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(3-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(3-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(3-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-aminophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-bromophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-butylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(4-nitrophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(furan-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(furan-3-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-(4-[4-[(naphthalen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-benzyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
-
 Homo sapiens
2.4.2.12 N-phenyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-4-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethoxy)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
-
 Homo sapiens
2.4.2.12 N-[(pyridin-3-yl)methyl]-N'-[4-[4-(pyridin-2-yl)piperazine-1-sulfonyl]phenyl]thiourea
-
 Homo sapiens
2.4.2.12 N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzothiophene-2-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-(4-acetylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-[4-(4-benzylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-[4-(4-cyclohexylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 N-[4-[(4E)-4-(2,3-dimethoxybenzylidene)-5-oxo-4,5-dihydro-1,3-oxazol-2-yl]phenyl]thiophene-2-carboxamide
-
 Homo sapiens
2.4.2.12 N-[4-[4-(4-methylphenyl)piperazine-1-sulfonyl]phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
 Homo sapiens
2.4.2.12 tert-butyl 4-[4-([[(pyridin-3-yl)methyl]carbamothioyl]amino)benzene-1-sulfonyl]piperazine-1-carboxylate
-
 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.4.2.12 55000
-
 x * 55000, SDS-PAGE 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
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.2.12 95-D cell
-
 Homo sapiens
-
2.4.2.12 A-2780 cell
-
 Homo sapiens
-
2.4.2.12 Hep-G2 cell
-
 Homo sapiens
-
2.4.2.12 U2OS 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
-
 ?

Subunits

EC Number Subunits Comment Organism
2.4.2.12 ? x * 55000, SDS-PAGE Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.4.2.12 Nampt
-
 Homo sapiens
2.4.2.12 pre-B cell colony enhancing factor
-
 Homo sapiens
2.4.2.12 Visfatin
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.12 0.0000009
-
 at pH 7.5 and 37°C Homo sapiens N-[4-(4-benzylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000089
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(3-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000098
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
2.4.2.12 0.0000099
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(2,6-difluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000105
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.000012
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000123
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(2-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000124
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(2-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000126
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(3-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000137
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000137
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-4-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
2.4.2.12 0.000014
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(1H-benzimidazol-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000142
-
 at pH 7.5 and 37°C Homo sapiens N-[4-(4-cyclohexylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000154
-
 at pH 7.5 and 37°C Homo sapiens N-[4-[4-(4-methylphenyl)piperazine-1-sulfonyl]phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000157
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(2-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000168
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(3-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000177
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-[4-[4-(pyridin-2-yl)piperazine-1-sulfonyl]phenyl]thiourea
2.4.2.12 0.0000191
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(furan-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000196
-
 at pH 7.5 and 37°C Homo sapiens N-benzyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
2.4.2.12 0.0000197
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-nitrophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000199
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-aminophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000201
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)urea
2.4.2.12 0.0000217
-
 at pH 7.5 and 37°C Homo sapiens tert-butyl 4-[4-([[(pyridin-3-yl)methyl]carbamothioyl]amino)benzene-1-sulfonyl]piperazine-1-carboxylate
2.4.2.12 0.0000217
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(morpholin-4-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
2.4.2.12 0.000022
-
 at pH 7.5 and 37°C Homo sapiens N-phenyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
2.4.2.12 0.0000225
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
2.4.2.12 0.0000237
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
2.4.2.12 0.0000242
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-bromophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000295
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(naphthalen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000369
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethoxy)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
2.4.2.12 0.0000388
-
 at pH 7.5 and 37°C Homo sapiens N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
2.4.2.12 0.0000405
-
 at pH 7.5 and 37°C Homo sapiens N-[4-(4-acetylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000422
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(piperidin-1-ylcarbonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
2.4.2.12 0.0000439
-
 at pH 7.5 and 37°C Homo sapiens 1-(pyridin-3-ylmethyl)-3-[4-(pyrrolidin-1-ylsulfonyl)phenyl]thiourea
2.4.2.12 0.0000487
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(furan-3-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000798
-
 at pH 7.5 and 37°C Homo sapiens N-(4-[4-[(4-butylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
2.4.2.12 0.0000845
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(piperazin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
2.4.2.12 0.0000964
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-(pyridin-3-ylmethyl)thiourea
2.4.2.12 0.0000989
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)urea
2.4.2.12 0.000765
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)guanidine
2.4.2.12 0.00987
-
 at pH 7.5 and 37°C Homo sapiens 1-[3-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
2.4.2.12 0.01453
-
 at pH 7.5 and 37°C Homo sapiens 1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)guanidine
2.4.2.12 0.149
-
 at pH 7.5 and 37°C Homo sapiens N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzothiophene-2-carboxamide
2.4.2.12 0.166
-
 at pH 7.5 and 37°C Homo sapiens ethyl [(E)-[4-(piperidine-1-sulfonyl)anilino][[(pyridin-3-yl)methyl]amino]methylidene]carbamate
2.4.2.12 0.504
-
 at pH 7.5 and 37°C Homo sapiens (2R,2'R)-5,5',7,7'-tetrahydroxy-2,2'-bis(4-hydroxyphenyl)-2,2',3,3'-tetrahydro-4H,4'H-[3,8'-bi-1-benzopyran]-4,4'-dione
2.4.2.12 0.855
-
 at pH 7.5 and 37°C Homo sapiens (1Z)-N'-(benzoyloxy)-3-(2-oxo-1,3-benzoxazol-3(2H)-yl)propanimidamide
2.4.2.12 4.162
-
 at pH 7.5 and 37°C Homo sapiens 4-chloro-N-[(5-[[(6-fluoro-4H-1,3-benzodioxin-8-yl)methyl]sulfamoyl]thiophen-2-yl)methyl]benzamide
2.4.2.12 6.443
-
 at pH 7.5 and 37°C Homo sapiens N-[4-[(4E)-4-(2,3-dimethoxybenzylidene)-5-oxo-4,5-dihydro-1,3-oxazol-2-yl]phenyl]thiophene-2-carboxamide