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

BRENDA support

BRENDA Home
show all | hide all No of entries

Information on EC 2.4.2.12 - nicotinamide phosphoribosyltransferase and Organism(s) Homo sapiens and UniProt Accession P43490

for references in articles please use BRENDA:EC2.4.2.12
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
     2 Transferases
         2.4 Glycosyltransferases
             2.4.2 Pentosyltransferases
                2.4.2.12 nicotinamide phosphoribosyltransferase
Specify your search results
Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: P43490 not found.
Show additional data
Do not include text mining results
Include (text mining) results
Include results (AMENDA + additional results, but less precise)
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
visfatin, nampt, nicotinamide phosphoribosyltransferase, enampt, nicotinamide phosphoribosyl transferase, naprt, pre-b-cell colony-enhancing factor, inampt, nampt/visfatin, nampt/pbef/visfatin, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
eNAMPT
extracellular nicotinamide phosphoribosyltrasferase
-
iNAMPT
intracellular enzyme
Nam phosphoribosyltransferase
-
Nampt/PBEF/Visfatin
-
nicotinamide phosphoribosyltransferase
-
pre-B cell colony-enhancing factor
-
pre-B colony enhancing factor
-
pre-B-cell colony enhancing factor
-
pre-B-cell colony-enhancing factor
-
NAmPRTase
-
-
-
-
NAPRT
-
-
nicotinamide mononucleotide pyrophosphorylase
-
-
-
-
nicotinamide mononucleotide synthetase
-
-
-
-
nicotinamide phosphoribosyl transferase
-
-
nicotinamide phosphoribosyltransferase
-
-
nicotinamide phosphoribosyltransferase/Visfatin
-
does not catalyze nicotinamide mononucleotide formation in blood plasma
NMN pyrophosphorylase
-
-
-
-
NMN synthetase
-
-
-
-
phosphoribosyltransferase, nicotinamide
-
-
-
-
pre-B cell colony enhancing factor
-
-
pre-B cell colony enhancing factor(PBEF)
-
-
pre-B cell colony-enhancing factor (PBEF)
-
-
pre-B-cell colony-enhancing factor
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pentosyl group transfer
pentosyl group transfer
-
-
-
-
PATHWAY SOURCE
PATHWAYS
-
-
SYSTEMATIC NAME
IUBMB Comments
nicotinamide-D-ribonucleotide:diphosphate phospho-alpha-D-ribosyltransferase
-
CAS REGISTRY NUMBER
COMMENTARY hide
9030-27-7
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ADP + ATP
ATP + ADP
show the reaction diagram
isotope exchange reaction (in presence of radiolabeled ADP and ATP but in absence of other reactants, meaning without NMN synthesis) requires high-energy phosphorylated NAMPT
-
-
r
ATP + H2O
ADP + phosphate
show the reaction diagram
DELTAG° = -7.3, in presence of NAMPT slow steady-state reaction after initial burst, ATPase activity in absence of other substrates, but can be modulated by addition of single substrates and mixtures
-
-
?
ATP + NAMPT
ADP + phospho-NAMPT
show the reaction diagram
autophosphorylation (DELTAG° = 1.9 kcal/mol, Keq = 0.047) is unfavourable and appears as initial burst of ADP generation
at 2.5 mM ATP and 46 microM NAMPT 77% of NAMPT is phosphorylated (proposed: His247 phospho-NAMPT), hydrolysis of phospho-NAMPT at 0.8/min, active phosphorylated NAMPT species neither isolated nor characterized yet
-
r
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
nicotinamide D-ribonucleotide + diphosphate
show the reaction diagram
nicotinamide + 5-phosphoribosyl 1-diphosphate
nicotinamide mononucleotide + diphosphate
show the reaction diagram
nicotinamide + alpha-D-5-phosphoribosyl 1-diphosphate
nicotinamide mononucleotide + diphosphate
show the reaction diagram
nicotinamide + alpha-D-5-phosphoribosyl 1-diphosphate + ATP + H2O
nicotinamide mononucleotide + diphosphate + ADP + phosphate
show the reaction diagram
DELTAG° = -1.0 kcal/mol, Keq = 5.0, reversion of the preestablished equilibrium in a non-ATP-coupled reaction, thermodynamic switch of the product-to-substrate ratio towards NMN production compared to the non-ATP-coupled reaction with an energy difference of -2.1 kcal/mol (meaning only 2.1 kcal/mol of 7.3 kcal/mol of the energy from ATP hydrolysis coupled to NMN formation), formation or hydrolysis of high-energy phosphorylated NAMPT may be rate limiting for overall ATP-coupled NMN synthesis
in presence of 2-2.5 mM ATP: 1 mol ADP per NMN formed (stoichiometric coupling ratio, R = 1), under optimal conditions (2 microM nicotinamide, 100 microM PRPP, 2.5 mM ATP, 5 mM Mg2+): R increases linearly with increasing diphosphate concentration
-
r
nicotinamide + alpha-D-5-phosphoribosyl-1-diphosphate
nicotinamide mononucleotide + diphosphate
show the reaction diagram
-
-
-
r
nicotinamide D-ribonucleotide + diphosphate
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
show the reaction diagram
-
-
-
?
phospho-NAMPT + H2O
NAMPT + phosphate
show the reaction diagram
DELTAG° = -9.2 kcal/mol
-
-
?
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
nicotinamide D-ribonucleotide + diphosphate
show the reaction diagram
nicotinamide + 5-phosphoribosyl 1-diphosphate
nicotinamide mononucleotide + diphosphate
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
nicotinamide D-ribonucleotide + diphosphate
show the reaction diagram
nicotinamide + alpha-D-5-phosphoribosyl 1-diphosphate
nicotinamide mononucleotide + diphosphate
show the reaction diagram
nicotinamide + alpha-D-5-phosphoribosyl-1-diphosphate
nicotinamide mononucleotide + diphosphate
show the reaction diagram
-
-
-
r
nicotinamide D-ribonucleotide + diphosphate
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
show the reaction diagram
-
-
-
?
nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate
nicotinamide D-ribonucleotide + diphosphate
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
10 mM used in assay conditions
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2E)-1-(4-[[2-(4-fluorophenyl)-1,3-thiazol-4-yl]methyl]piperazin-1-yl)-3-(pyridin-3-yl)prop-2-en-1-one
-
(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
(2E)-3-(pyridin-3-yl)-1-[4-[4-(trifluoromethoxy)benzyl]piperazin-1-yl]prop-2-en-1-one
-
(2E)-3-(pyridin-3-yl)-N-[4-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)phenyl]prop-2-enamide
-
(2E)-3-(pyridin-3-yl)-N-[6-(3-[[4-(trifluoromethyl)phenyl]sulfamoyl]phenyl)hexyl]prop-2-enamide
-
(2E)-N-(6-[3-[(2,5-dimethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(2-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
most potent inhibitor
(2E)-N-(6-[3-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(3-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(4-chlorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(4-ethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(4-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(4-phenoxyphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-(6-[3-[(4-tert-butylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[2-[(2,2-dimethyl-2,3-dihydro-1-benzofuran-6-yl)oxy]ethyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[3-(1H-imidazol-1-yl)propyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[3-[3-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[3-[4-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide
(2E)-N-[4-[4-(phenylsulfamoyl)phenyl]butyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[5-[3-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[5-[4-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[5-[4-([[2-(1H-indol-3-yl)ethyl](propan-2-yl)amino]methyl)anilino]pentyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[6-[3-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[6-[4-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[7-[3-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
-
(2E)-N-[7-[4-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
-
(3R,5R,7R)-N-(4-((E)-3-(pyridin-3-yl)acrylamido)butyl)adamantane-1-carboxamide
-
(E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidepentyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(1,7-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(1-(1,12-dicarba-closo-dodecaboranyl)piperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(1-benzoyl-1,12-dicarba-closo-dodecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(1-trimethylsilyl-1,12-dicarba-closododecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,7-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranyl(hydroxy)methyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
(E)-N-(4-(4-(1,7-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
-
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
-
1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,12-dicarba-closo-dodecaborane
-
1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,2-dicarba-closo-dodecaborane
-
1-((E)-4-(3-(pyridin-3-yl)acrylamido)pentyl)-1,2-dicarba-closo-dodecaborane
-
1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)butyl)-1,2-dicarba-closo-dodecaborane
-
1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)pentyl)-1,2-dicarba-closo-dodecaborane
-
1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)butyl)-1,2-dicarba-closo-dodecaborane
-
1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)pentyl)-1,2-dicarba-closo-dodecaborane
-
1-methyl-N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
-
1-[2-(naphthalen-2-yloxy)ethyl]-3-(pyridin-3-ylmethyl)urea
-
1-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)urea
-
1H-indol-2-yl(4-[[3-(pyridin-3-yl)-1H-pyrazol-5-yl]carbonyl]piperazin-1-yl)methanone
-
2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-2-carboxylic acid
-
2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-3-carboxylic acid
-
2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-4-carboxylic acid
-
2'-methyl-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
-
2'-[(aminooxy)carbonyl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
-
2-(4-[[4-(1-ethoxyethenyl)piperidin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-(4-[[4-(propan-2-yl)piperazin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)ethyl [1,1'-biphenyl]-2-ylcarbamate
-
2-(4-[[bis(2-hydroxyethyl)amino]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-(pyridin-3-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-bromo-N-[2-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)ethyl]benzene-1-sulfonamide
-
2-cyano-1-[4-(phenylsulfonyl)benzyl]-3-pyridin-4-ylguanidine
-
2-[4-[(4-chlorophenyl)sulfamoyl]phenoxy]-N-(pyridin-3-ylmethyl)acetamide
-
2-[4-[(4-hydroxypiperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-[4-[(4-methylpiperazin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
inhibitor of the extracellular enzyme form
2-[4-[(dimethylamino)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-[4-[(morpholin-4-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
2-[4-[(piperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
-
3-(1-[6-[(2'-methyl[1,1'-biphenyl]-2-yl)oxy]hexyl]-1H-1,2,3-triazol-4-yl)pyridine
-
3-(1-[6-[([1,1'-biphenyl]-2-yl)oxy]hexyl]-1H-1,2,3-triazol-4-yl)pyridine
-
3-(1-[6-[2-(pyridin-3-yl)phenoxy]hexyl]-1H-1,2,3-triazol-4-yl)pyridine
-
3-(1-[7-[([1,1'-biphenyl]-2-yl)oxy]heptyl]-1H-1,2,3-triazol-4-yl)pyridine
-
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
-
3-(1-[8-[([1,1'-biphenyl]-2-yl)oxy]octyl]-1H-1,2,3-triazol-4-yl)pyridine
-
3-[1-[(4-[2-[([1,1'-biphenyl]-2-yl)oxy]ethyl]phenyl)methyl]-1H-1,2,3-triazol-4-yl]pyridine
-
4-chloro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
4-[([7-chloro-3-methyl-2-[(4-methylpiperazin-1-yl)methyl]-4-oxo-3,4-dihydroquinazolin-6-yl]methyl)(prop-2-yn-1-yl)amino]-N-[(pyridin-3-yl)methyl]benzamide
-
4-[[(2E)-3-(pyridin-3-yl)prop-2-enoyl]amino]-N-(2,2,2-trifluoroethyl)benzamide
-
4-[[(3,7-dimethyl-4-oxo-3,4-dihydro-1,2,3-benzotriazin-6-yl)methyl](3-methylbut-2-en-1-yl)amino]-N-[(pyridin-3-yl)methyl]benzamide
-
4-[[(4-tert-butylbenzene-1-sulfonyl)amino]methyl]-N-(pyridin-3-yl)benzamide
-
5,6-dimethoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-(3,4-dichlorobenzyl)-4-oxo-N-(pyridin-3-ylmethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamide
-
5-(hydroxymethyl)-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-chloro-N-(4-[1-[(2S)-oxolane-2-carbonyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-cyano-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-fluoro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-fluoro-N-[4-[1-(1-methylpiperidine-4-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-fluoro-N-[4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-methoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5-methyl-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
5P-DADMe-NMN
poor, competitive inhibitor of non-ATP and ATP coupled NMN synthesis with respect to PRPP and nicotinamide, 3-fold increased binding in presence of ATP
6-[(benzylcarbamoyl)amino]-N-cyclohexyl-N-[2-(morpholin-4-yl)ethoxy]hexane-1-sulfonamide
-
6-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]hexyl [1,1'-biphenyl]-2-ylcarbamate
-
7-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)heptyl [1,1'-biphenyl]-2-ylcarbamate
-
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
-
alpha-D-5-phosphoribosyl 1-diphosphate
inhibits ATPase activity at 1 mM concentration, nearly complete inhibition of ADP-ATP exchange at 100 microM
APO866
CHS-828
competitive inhibitor
CHS828
FK-866
GMX-1778
methyl 4-[(1,3-dihydro-2H-isoindole-2-carbonyl)amino]benzoate
-
N''-cyano-N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-N'-pyridin-4-ylguanidine
-
N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethoxy)benzene-1-sulfonyl]phenyl]methyl)guanidine
-
N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethyl)benzene-1-sulfonyl]phenyl]methyl)guanidine
-
N''-cyano-N-pyridin-4-yl-N'-[[4-(quinoline-8-sulfonyl)phenyl]methyl]guanidine
-
N''-cyano-N-[[4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
N''-cyano-N-[[4-(3-methoxybenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-3-ylguanidine
-
N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
N''-cyano-N-[[4-(cyclohexanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
N''-cyano-N-[[4-(phenylmethanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
N''-cyano-N-[[4-(pyridine-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
-
N-(2-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-oxoethyl)-3-methylthiophene-2-carboxamide
-
N-(2-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-oxoethyl)-5-methylthiophene-2-carboxamide
-
N-(4-butylphenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-methylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-[1-[2-methyl-2-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-[3-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]propyl]phenyl)[1,1'-biphenyl]-2-carboxamide
-
N-(4-[[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-[[(oxan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-[[(oxolan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-[[1-(2-methylbutanoyl)piperidin-4-yl]oxy]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-(4-[[1-(propan-2-yl)-1H-pyrazol-4-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-(4-[[3-(trifluoromethoxy)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-(4-[[3-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
N-(4-[[4-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-(4-[[5-(trifluoromethyl)pyridin-3-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-(7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl)[1,1'-biphenyl]-2-carboxamide
MV78
N-(pyridin-4-yl)cyclopropanecarboxamide
-
N-([1,1'-biphenyl]-2-yl)-8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octanamide
N-([4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl)imidazo[1,2-a]pyridine-6-carboxamide
GNE-617
N-([4-[(3,5-difluorophenyl)methyl]phenyl]methyl)imidazo[1,2-a]pyridine-6-carboxamide
-
N-([4-[1-(oxan-4-yl)piperidine-4-sulfonyl]phenyl]methyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
N-([4-[4-(oxetan-3-yl)piperazine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-([4-[4-(pyrrolidin-1-yl)piperidine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-([4-[6-(dimethylamino)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-biphenyl-2-yl-8-(4-pyridin-3-yl-1H-1,2,3-triazol-1-yl)octanamide
displays an IC50 for cytotoxicity in vitro of 3.8 nM and an IC50 for NAD depletion of 3.0 nM. Compound induces autophagic cell death
-
N-[(5-[[3-(trifluoromethyl)phenyl]sulfonyl]pyridin-2-yl)methyl]furo[2,3-c]pyridine-2-carboxamide
-
N-[([1,1'-biphenyl]-2-yl)methyl]-2-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)ethan-1-amine
-
N-[1,1'-biphenyl]-2-yl-N'-[2-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)ethyl]urea
-
N-[1,1'-biphenyl]-2-yl-N'-[6-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]hexyl]urea
-
N-[1,1'-biphenyl]-2-yl-N'-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]urea
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzofuran-2-carboxamide
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzothiophene-2-carboxamide
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-3-methylthiophene-2-carboxamide
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-5-methylthiophene-2-carboxamide
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-5-nitrothiophene-2-carboxamide
-
N-[2-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)ethyl][1,1'-biphenyl]-2-carboxamide
-
N-[2-(4-[[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]methyl]phenyl)ethyl][1,1'-biphenyl]-2-sulfonamide
-
N-[2-chloro-5-(trifluoromethyl)phenyl]-4-([[(pyridin-3-yl)methyl]carbamoyl]amino)benzene-1-sulfonamide
-
N-[3-(1H-imidazol-1-yl)propyl]-1-benzofuran-2-carboxamide
-
N-[3-(1H-imidazol-1-yl)propyl]-1-benzothiophene-2-carboxamide
-
N-[3-(1H-imidazol-1-yl)propyl]-3-methylthiophene-2-carboxamide
-
N-[3-(1H-imidazol-1-yl)propyl]-5-methylthiophene-2-carboxamide
-
N-[3-(1H-imidazol-1-yl)propyl]-5-nitrothiophene-2-carboxamide
-
N-[3-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(1-benzoylazetidin-3-yl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(1-propyl-1H-pyrazole-3-sulfonyl)phenyl]-2-(pyridin-3-yl)cyclopropane-1-carboxamide
-
N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]urea
-
N-[4-(benzenesulfonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(benzenesulfonyl)phenyl]-2-(pyridin-3-yl)cyclopropane-1-carboxamide
-
N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(morpholin-4-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-c]pyridine-5-carboxamide
-
N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
-
N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide
-
N-[4-(phenylsulfonyl)benzyl]-5-(pyridin-3-yl)-1H-pyrazole-3-carboxamide
-
N-[4-(phenylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
-
N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-indazole-5-carboxamide
-
N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-(piperidin-1-ylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
-
N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-(quinolin-3-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-([[(3S)-oxolan-3-yl]methyl]carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(1-ethyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-[(1-propyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-[(3,3-dimethylbutyl)(methyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(3,3-dimethylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]imidazo[1,2-a]pyridine-6-carboxamide
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(3-methylbutyl)sulfamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(3-phenylpropyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(4-cyanopiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-[(4-hydroxypiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-[(4-methylpentanoyl)amino]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[(5-chloropyridin-3-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[4-[(6-methylpyridin-3-yl)sulfonyl]benzyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
N-[4-[1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[1-(3-methyloxetane-3-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[1-(cyclopropanesulfonyl)piperidin-4-yl]phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[4-[4-(pyridin-2-yl)piperazine-1-carbonyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[5-[(3-methylbutyl)carbamoyl]pyridin-2-yl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[6-(4-chlorophenoxy)hexyl]-N''-cyano-N'-phenylguanidine
CHS828
N-[6-[(3-methylbutyl)carbamoyl]pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[6-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]hexyl][1,1'-biphenyl]-2-carboxamide
-
N-[7-[4-(1-oxo-1lambda(5)-pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
-
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-1-yl)benzamide
inhibitor of the intracellular enzyme form
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-4-yl)benzamide
-
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-[4-[(pyrrolidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]benzamide
-
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
-
N-[8-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]octyl][1,1'-biphenyl]-2-sulfonamide
-
N-[[4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
-
N-[[4-(4-aminopiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[[4-(4-methoxypiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[[4-(6-methylpyridine-3-sulfonyl)phenyl]methyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
-
N-[[4-(7-oxa-2-azaspiro[3.5]nonane-2-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
-
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,3-dihydro-2H-isoindole-2-carboxamide
-
N-[[4-(benzenesulfonyl)phenyl]methyl]-1H-pyrazolo[4,3-b]pyridine-5-carboxamide
-
N-[[4-(benzenesulfonyl)phenyl]methyl]-N''-cyano-N'-pyridin-3-ylguanidine
-
NAD+
competitive inhibitor of non-ATP and ATP coupled NMN synthesis with respect to PRPP and nicotinamide
NADH
competitive inhibitor of non-ATP and ATP coupled NMN synthesis with respect to PRPP and nicotinamide
nicotinamide
substrate inhibition
teglarinad
water soluble pro-drug of N-[6-(4-chlorophenoxy)hexyl]-N''-cyano-N'-phenylguanidine (CHS828)
tert-butyl ((1,12-dicarba-closo-dodecaboranylamido)propyl)carbamate
-
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
-
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
-
TP201565
competitive inhibitor
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
potent inhibitor
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
-
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
-
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
-
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
-
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
-
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
-
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
-
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
-
[4-(diphenylmethyl)piperazin-1-yl][5-(pyridin-3-yl)-1H-pyrazol-3-yl]methanone
-
(1Z)-N'-(benzoyloxy)-3-(2-oxo-1,3-benzoxazol-3(2H)-yl)propanimidamide
-
-
(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
-
-
1-(pyridin-3-ylmethyl)-3-[4-(pyrrolidin-1-ylsulfonyl)phenyl]thiourea
-
-
1-[3-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
potent inhibitor
1-[4-(morpholin-4-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
-
1-[4-(piperazin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
-
1-[4-(piperidin-1-ylcarbonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
-
1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)guanidine
-
-
1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)urea
-
-
1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)guanidine
-
-
1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)urea
-
-
1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-4-ylmethyl)thiourea
-
-
1-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-(pyridin-3-ylmethyl)thiourea
-
-
4-chloro-N-[(5-[[(6-fluoro-4H-1,3-benzodioxin-8-yl)methyl]sulfamoyl]thiophen-2-yl)methyl]benzamide
-
-
ethyl [(E)-[4-(piperidine-1-sulfonyl)anilino][[(pyridin-3-yl)methyl]amino]methylidene]carbamate
-
-
FK-866
-
i.e. (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-phenylprop-2-enamide
FK866
GMX1777
-
i.e. 1-[2-(2-(2-(2-methoxyethoxy)-ethoxy)ethoxy)-ethoxy-carbonyloxymethyl]-4-[N'-cyano-N''-(6-(4-chlorophenyl)-hexyl)-N-guanidino]pyridinium chloride, prodrug of GMX1778. A dose of 75 mg/kg administered over a 24 h intravenous infusion causes tumor regression in the IM-9 model, the SHP-77 model, and HCT-116 model. A 72 h continuous intravenous infusion is also effective in the IM-9 model, but is associated with smaller therapeutic index
hypoxanthine
-
phosphorolysis
N-(4-[4-[(1H-benzimidazol-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(2,6-difluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(2-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(2-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(2-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(3-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(3-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(3-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-aminophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-bromophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-butylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(4-nitrophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(furan-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(furan-3-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-(4-[4-[(naphthalen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-benzyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
-
-
N-phenyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
-
-
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
-
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-4-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
-
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
-
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
-
-
N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethoxy)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
-
-
N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
-
-
N-[(pyridin-3-yl)methyl]-N'-[4-[4-(pyridin-2-yl)piperazine-1-sulfonyl]phenyl]thiourea
-
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzothiophene-2-carboxamide
-
-
N-[4-(4-acetylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-[4-(4-benzylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-[4-(4-cyclohexylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
-
N-[4-[(4E)-4-(2,3-dimethoxybenzylidene)-5-oxo-4,5-dihydro-1,3-oxazol-2-yl]phenyl]thiophene-2-carboxamide
-
-
N-[4-[4-(4-methylphenyl)piperazine-1-sulfonyl]phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
-
-
NAD+
-
-
nicotinate adenine dinucleotide
-
not inhibitory
tert-butyl 4-[4-([[(pyridin-3-yl)methyl]carbamothioyl]amino)benzene-1-sulfonyl]piperazine-1-carboxylate
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
ATP
35-fold higher concentrations of NMN synthesised, impact on substrate affinities, coupling of ATP hydrolysis to NMN synthesis enhances catalytic efficiency, accelerates forward turnover and overcomes the unfavourable thermodynamic equilibrium
diphosphate
enhanced ATPase activity
nicotinamide
enhanced ATPase activity
ATP
-
essential activator
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.44
ADP
+/-0.05 mM, ADP-ATP radiolabel exchange in absence of other reactants
0.00063 - 0.0117
alpha-D-5-phosphoribosyl 1-diphosphate
2.2 - 7.4
ATP
0.000005 - 0.000855
nicotinamide
0.18
phosphate
+/-0.02 mM, pH 7.5, 88 nM NAMPT, HPLC-based quantification
0.00537
5-phospho-alpha-D-ribose 1-diphosphate
-
-
0.00051 - 0.0232
5-phosphoribosyl 1-diphosphate
0.00122 - 100
nicotinamide
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0003 - 0.0433
ATP
0.00137 - 0.00767
nicotinamide
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000017
4-chloro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.009
5,6-dimethoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
Ki above 0.009 mM, pH and temperature not specified in the publication
0.0000049
5-(hydroxymethyl)-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000017
5-chloro-N-(4-[1-[(2S)-oxolane-2-carbonyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000047
5-cyano-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000079
5-fluoro-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000094
5-fluoro-N-[4-[1-(1-methylpiperidine-4-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000025
5-fluoro-N-[4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000016
5-methoxy-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000013
5-methyl-N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.00016 - 0.0071
5P-DADMe-NMN
0.000003
FK866
pH and temperature not specified in the publication
0.000003
GMX1778
pH and temperature not specified in the publication
0.000112
methyl 4-[(1,3-dihydro-2H-isoindole-2-carbonyl)amino]benzoate
pH and temperature not specified in the publication
0.00056
N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0022
N-(4-methylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000015
N-(4-[1-[2-methyl-2-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000019
N-(4-[[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000013
N-(4-[[(oxan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000024
N-(4-[[(oxolan-3-yl)methyl]carbamoyl]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000018
N-(4-[[1-(2-methylbutanoyl)piperidin-4-yl]oxy]phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0089
N-[3-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
Ki above 0.0089 mM, pH and temperature not specified in the publication
0.000003
N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000019
N-[4-(1-benzoylazetidin-3-yl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000016
N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000001
N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000019
N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000021
N-[4-(benzenesulfonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000019
N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000104
N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.00016
N-[4-[(3,3-dimethylbutyl)(methyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000014
N-[4-[(3,3-dimethylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000011
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000075
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide
pH and temperature not specified in the publication
0.000023
N-[4-[(3-methylbutyl)carbamoyl]phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.00035
N-[4-[(3-methylbutyl)sulfamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000009
N-[4-[(3-phenylpropyl)carbamoyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000058
N-[4-[(4-methylpentanoyl)amino]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000043
N-[4-[1-(1-methylcyclopropane-1-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000015
N-[4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000056
N-[4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000023
N-[4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000051
N-[4-[1-(3-methyloxetane-3-carbonyl)piperidin-4-yl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000039
N-[4-[1-(cyclopropanesulfonyl)piperidin-4-yl]phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000014
N-[4-[4-(pyridin-2-yl)piperazine-1-carbonyl]phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.0000054
N-[5-[(3-methylbutyl)carbamoyl]pyridin-2-yl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000057
N-[6-[(3-methylbutyl)carbamoyl]pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.000487
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,3-dihydro-2H-isoindole-2-carboxamide
pH and temperature not specified in the publication
0.00014 - 0.0021
NAD+
0.00022 - 0.0032
NADH
0.00025 - 0.003
nicotinamide
0.0003 - 0.0004
FK866
additional information
ATP
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0032
(2E)-1-(4-[[2-(4-fluorophenyl)-1,3-thiazol-4-yl]methyl]piperazin-1-yl)-3-(pyridin-3-yl)prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00078
(2E)-3-(pyridin-3-yl)-1-[4-[4-(trifluoromethoxy)benzyl]piperazin-1-yl]prop-2-en-1-one
Homo sapiens
pH and temperature not specified in the publication
0.00067
(2E)-3-(pyridin-3-yl)-N-[4-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)phenyl]prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00002453
(2E)-3-(pyridin-3-yl)-N-[6-(3-[[4-(trifluoromethyl)phenyl]sulfamoyl]phenyl)hexyl]prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001163
(2E)-N-(6-[3-[(2,5-dimethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00000508
(2E)-N-(6-[3-[(2-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.0000097
(2E)-N-(6-[3-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001228
(2E)-N-(6-[3-[(3-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001075
(2E)-N-(6-[3-[(4-chlorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00003154
(2E)-N-(6-[3-[(4-ethylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.0000092
(2E)-N-(6-[3-[(4-fluorophenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00000978
(2E)-N-(6-[3-[(4-methylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001309
(2E)-N-(6-[3-[(4-phenoxyphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00000947
(2E)-N-(6-[3-[(4-tert-butylphenyl)sulfamoyl]phenyl]hexyl)-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.01
(2E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00094
(2E)-N-[2-[(2,2-dimethyl-2,3-dihydro-1-benzofuran-6-yl)oxy]ethyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.01
(2E)-N-[3-(1H-imidazol-1-yl)propyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.0002345
(2E)-N-[3-[3-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00592
(2E)-N-[3-[4-(phenylsulfamoyl)phenyl]propyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.0000027
(2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001777
(2E)-N-[4-[4-(phenylsulfamoyl)phenyl]butyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001654
(2E)-N-[5-[3-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00002839
(2E)-N-[5-[4-(phenylsulfamoyl)phenyl]pentyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001053
(2E)-N-[6-[3-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001442
(2E)-N-[6-[4-(phenylsulfamoyl)phenyl]hexyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00003132
(2E)-N-[7-[3-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.00001641
(2E)-N-[7-[4-(phenylsulfamoyl)phenyl]heptyl]-3-(pyridin-3-yl)prop-2-enamide
Homo sapiens
pH and temperature not specified in the publication
0.008
(3R,5R,7R)-N-(4-((E)-3-(pyridin-3-yl)acrylamido)butyl)adamantane-1-carboxamide
Homo sapiens
at 30°C, pH not specified in the publication
0.000057
(E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.00017
(E)-N-(4-(1,12-dicarba-closo-dodecaboranyl)amidepentyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.000098
(E)-N-(4-(1,7-dicarba-closo-dodecaboranyl)amidebutyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.00032
(E)-N-(4-(1-(1,12-dicarba-closo-dodecaboranyl)piperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.00063
(E)-N-(4-(1-benzoyl-1,12-dicarba-closo-dodecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.00018
(E)-N-(4-(1-trimethylsilyl-1,12-dicarba-closododecaboran-12-yl)amidebutyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.01
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
IC50 above 0.01 mM, at 30°C, pH not specified in the publication
0.00292
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranecarbonyl)-1,7-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.00451
(E)-N-(4-(4-(1,12-dicarba-closo-dodecaboranyl(hydroxy)methyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.00376
(E)-N-(4-(4-(1,7-dicarba-closo-dodecaboranecarbonyl)-1,12-dicarba-closo-dodecaboranyl)butyl)-3-(pyridin-3-yl)acrylamide
Homo sapiens
at 30°C, pH not specified in the publication
0.000062
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
pH and temperature not specified in the publication
0.00025
1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,12-dicarba-closo-dodecaborane
Homo sapiens
at 30°C, pH not specified in the publication
0.00037
1-((E)-4-(3-(pyridin-3-yl)acrylamido)hexyl)-1,2-dicarba-closo-dodecaborane
Homo sapiens
at 30°C, pH not specified in the publication
0.0049
1-((E)-4-(3-(pyridin-3-yl)acrylamido)pentyl)-1,2-dicarba-closo-dodecaborane
Homo sapiens
at 30°C, pH not specified in the publication
0.03
1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)butyl)-1,2-dicarba-closo-dodecaborane
Homo sapiens
IC50 above 0.03 mM, at 30°C, pH not specified in the publication
0.03
1-(4-(4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl)pentyl)-1,2-dicarba-closo-dodecaborane
Homo sapiens
IC50 above 0.03 mM, at 30°C, pH not specified in the publication
0.03
1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)butyl)-1,2-dicarba-closo-dodecaborane
Homo sapiens
IC50 above 0.03 mM, at 30°C, pH not specified in the publication
0.03
1-(5-(1H-pyrrolo[3,2-c]pyridine-2-carboxamido)pentyl)-1,2-dicarba-closo-dodecaborane
Homo sapiens
IC50 above 0.03 mM, at 30°C, pH not specified in the publication
0.002
1-methyl-N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000003
1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea
Homo sapiens
pH and temperature not specified in the publication
0.005
1-[2-(naphthalen-2-yloxy)ethyl]-3-(pyridin-3-ylmethyl)urea
Homo sapiens
pH and temperature not specified in the publication
0.0038
1H-indol-2-yl(4-[[3-(pyridin-3-yl)-1H-pyrazol-5-yl]carbonyl]piperazin-1-yl)methanone
Homo sapiens
pH and temperature not specified in the publication
0.0000385
2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.0005
2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
IC50 above 0.0005 mM, pH and temperature not specified in the publication
0.0005
2'-([7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]carbamoyl)[1,1'-biphenyl]-4-carboxylic acid
Homo sapiens
IC50 above 0.0005 mM, pH and temperature not specified in the publication
0.0000879
2'-[(aminooxy)carbonyl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000206
2-(4-[[4-(1-ethoxyethenyl)piperidin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000247
2-(4-[[4-(propan-2-yl)piperazin-1-yl]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000738
2-(4-[[bis(2-hydroxyethyl)amino]methyl]-1H-1,2,3-triazol-1-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000285
2-(pyridin-3-yl)-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000025
2-cyano-1-[4-(phenylsulfonyl)benzyl]-3-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0019
2-[4-[(4-chlorophenyl)sulfamoyl]phenoxy]-N-(pyridin-3-ylmethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000418
2-[4-[(4-hydroxypiperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000136
2-[4-[(4-methylpiperazin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000424
2-[4-[(dimethylamino)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000496
2-[4-[(morpholin-4-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000171
2-[4-[(piperidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]-N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00022
4-[[(2E)-3-(pyridin-3-yl)prop-2-enoyl]amino]-N-(2,2,2-trifluoroethyl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00032
5-(3,4-dichlorobenzyl)-4-oxo-N-(pyridin-3-ylmethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.23
7-chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Homo sapiens
pH and temperature not specified in the publication
0.00011 - 0.008585
FK-866
0.0000068 - 0.00062
FK866
0.0000017
N''-cyano-N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000044
N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethoxy)benzene-1-sulfonyl]phenyl]methyl)guanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000024
N''-cyano-N-pyridin-4-yl-N'-([4-[3-(trifluoromethyl)benzene-1-sulfonyl]phenyl]methyl)guanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000036
N''-cyano-N-pyridin-4-yl-N'-[[4-(quinoline-8-sulfonyl)phenyl]methyl]guanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000006
N''-cyano-N-[[4-(3,5-difluorobenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000019
N''-cyano-N-[[4-(3-methoxybenzene-1-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000044
N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-3-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000024
N''-cyano-N-[[4-(8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000054
N''-cyano-N-[[4-(cyclohexanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.0000075
N''-cyano-N-[[4-(phenylmethanesulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.000002
N''-cyano-N-[[4-(pyridine-3-sulfonyl)phenyl]methyl]-N'-pyridin-4-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.01
N-(2-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-oxoethyl)-3-methylthiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00095
N-(2-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-oxoethyl)-5-methylthiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000418
N-(4-butylphenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000099
N-(4-[[1-(propan-2-yl)-1H-pyrazol-4-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000077
N-(4-[[3-(trifluoromethoxy)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000061
N-(4-[[3-(trifluoromethyl)phenyl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
N-(4-[[5-(trifluoromethyl)pyridin-3-yl]sulfonyl]benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000031
N-(7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl)[1,1'-biphenyl]-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.002
N-(pyridin-4-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00044
N-([4-[4-(oxetan-3-yl)piperazine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0003
N-([4-[4-(pyrrolidin-1-yl)piperidine-1-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
N-([4-[6-(dimethylamino)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000045
N-([4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl]methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0014
N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzofuran-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00015
N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzothiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0053
N-[2-(3,4-dimethoxyphenyl)ethyl]-3-methylthiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00086
N-[2-(3,4-dimethoxyphenyl)ethyl]-5-methylthiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.01
N-[2-(3,4-dimethoxyphenyl)ethyl]-5-nitrothiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.001
N-[3-(1H-imidazol-1-yl)propyl]-1-benzofuran-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0011
N-[3-(1H-imidazol-1-yl)propyl]-1-benzothiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.01
N-[3-(1H-imidazol-1-yl)propyl]-3-methylthiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00017
N-[3-(1H-imidazol-1-yl)propyl]-5-methylthiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.01
N-[3-(1H-imidazol-1-yl)propyl]-5-nitrothiophene-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000051
N-[4-(1-propyl-1H-pyrazole-3-sulfonyl)phenyl]-2-(pyridin-3-yl)cyclopropane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00037
N-[4-(morpholin-4-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000066
N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.002
N-[4-(phenylsulfonyl)benzyl]-1H-pyrazolo[3,4-c]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.002
N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000029
N-[4-(phenylsulfonyl)benzyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000043
N-[4-(phenylsulfonyl)benzyl]-5-(pyridin-3-yl)-1H-pyrazole-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.018
N-[4-(phenylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.002
N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-indazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000088
N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.028
N-[4-(piperidin-1-ylsulfonyl)benzyl]imidazo[1,2-a]pyridine-6-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000082
N-[4-(quinolin-3-ylsulfonyl)benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00019
N-[4-[(1-ethyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
N-[4-[(1-propyl-1H-pyrazol-4-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000079
N-[4-[(3,5-difluorophenyl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00041
N-[4-[(4-cyanopiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00041
N-[4-[(4-hydroxypiperidin-1-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000011
N-[4-[(5-chloropyridin-3-yl)sulfonyl]benzyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0005
N-[7-[4-(1-oxo-1lambda(5)-pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl][1,1'-biphenyl]-2-carboxamide
Homo sapiens
IC50 above 0.0005 mM, pH and temperature not specified in the publication
0.0000034
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000425
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-(1H-1,2,3-triazol-4-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000254
N-[7-[4-(pyridin-3-yl)-1H-1,2,3-triazol-1-yl]heptyl]-2-[4-[(pyrrolidin-1-yl)methyl]-1H-1,2,3-triazol-1-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00039
N-[[4-(4-aminopiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0004
N-[[4-(4-methoxypiperidine-1-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00011
N-[[4-(7-oxa-2-azaspiro[3.5]nonane-2-sulfonyl)phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000063
N-[[4-(benzenesulfonyl)phenyl]methyl]-1,1-dioxo-2H-pyrido[4,3-e][1,2,4]thiadiazin-3-amine
Homo sapiens
pH and temperature not specified in the publication
0.0013
N-[[4-(benzenesulfonyl)phenyl]methyl]-1H-pyrazolo[4,3-b]pyridine-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000022
N-[[4-(benzenesulfonyl)phenyl]methyl]-N''-cyano-N'-pyridin-3-ylguanidine
Homo sapiens
pH and temperature not specified in the publication
0.03
tert-butyl ((1,12-dicarba-closo-dodecaboranylamido)propyl)carbamate
Homo sapiens
IC50 above 0.03 mM, at 30°C, pH not specified in the publication
0.002
tert-butyl trans-1-(2-(pyridin-3-yl)cyclopropanecarbonyl)-hexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.002
tert-butyl trans-6-(2-(pyridin-3-yl)cyclopropanecarbonyl)-2,6-diazaspiro[3.4]octane-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.00046
trans-(R,R)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
trans-(S,S)-N-(4-((1-isopropyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000051
trans-(S,S)-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.002
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)benzyl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000049
trans-2-(6-aminopyridin-3-yl)-N-(4-(phenylsulfonyl)phenyl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
trans-2-(pyridin-3-yl)-N-(4-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000066
trans-2-(pyridin-3-yl)-N-(4-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)sulfonyl)phenyl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000095
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethoxy)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
trans-2-(pyridin-3-yl)-N-(4-((3-(trifluoromethyl)phenyl)-sulfonyl)phenyl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000036
trans-2-(pyridin-3-yl)-N-(4-((tetrahydro-2H-pyran-4-yl)-sulfonyl)phenyl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0016
trans-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
trans-N-(4-((1-(2-Hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000009
trans-N-(4-((1-ethyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
trans-N-(4-((1-Isopropyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000038
trans-N-(4-((1-isopropyl-3-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000011
trans-N-(4-((1-isopropyl-5-methyl-1H-pyrazol-4-yl)sulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000072
trans-N-(4-((1-propyl-1H-pyrazol-4-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
trans-N-(4-((3,5-difluorophenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000044
trans-N-(4-((3-(methylsulfonyl)phenyl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
trans-N-(4-((6-methylpyridin-3-yl)sulfonyl)phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000047
trans-N-(4-(1-benzoylpiperidin-4-yl)butyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000088
trans-N-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)-phenyl)-2-(pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000021
trans-N-(4-(morpholinosulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0015
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.002
trans-N-(4-(phenylsulfonyl)benzyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000078
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0013
trans-N-(4-(phenylsulfonyl)phenyl)-2-(pyridin-4-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000076
trans-N-(6-(4-chlorophenoxy)hexyl)-2-(pyridin-3-yl)-cyclopropanecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0002427
[4-(diphenylmethyl)piperazin-1-yl][5-(pyridin-3-yl)-1H-pyrazol-3-yl]methanone
Homo sapiens
pH and temperature not specified in the publication
0.855
(1Z)-N'-(benzoyloxy)-3-(2-oxo-1,3-benzoxazol-3(2H)-yl)propanimidamide
Homo sapiens
-
at pH 7.5 and 37°C
0.504
(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
-
at pH 7.5 and 37°C
0.0000439
1-(pyridin-3-ylmethyl)-3-[4-(pyrrolidin-1-ylsulfonyl)phenyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.00987
1-[3-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000217
1-[4-(morpholin-4-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000845
1-[4-(piperazin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000422
1-[4-(piperidin-1-ylcarbonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.01453
1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)guanidine
Homo sapiens
-
at pH 7.5 and 37°C
0.0000989
1-[4-(piperidin-1-yloxy)phenyl]-3-(pyridin-3-ylmethyl)urea
Homo sapiens
-
at pH 7.5 and 37°C
0.000765
1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)guanidine
Homo sapiens
-
at pH 7.5 and 37°C
0.0000201
1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)urea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000964
1-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-(pyridin-3-ylmethyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
4.162
4-chloro-N-[(5-[[(6-fluoro-4H-1,3-benzodioxin-8-yl)methyl]sulfamoyl]thiophen-2-yl)methyl]benzamide
Homo sapiens
-
at pH 7.5 and 37°C
0.166
ethyl [(E)-[4-(piperidine-1-sulfonyl)anilino][[(pyridin-3-yl)methyl]amino]methylidene]carbamate
Homo sapiens
-
at pH 7.5 and 37°C
0.000014
N-(4-[4-[(1H-benzimidazol-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000099
N-(4-[4-[(2,6-difluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000157
N-(4-[4-[(2-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000123
N-(4-[4-[(2-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000124
N-(4-[4-[(2-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000126
N-(4-[4-[(3-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000089
N-(4-[4-[(3-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000168
N-(4-[4-[(3-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000199
N-(4-[4-[(4-aminophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000242
N-(4-[4-[(4-bromophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000798
N-(4-[4-[(4-butylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000137
N-(4-[4-[(4-chlorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.000012
N-(4-[4-[(4-fluorophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000105
N-(4-[4-[(4-methylphenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000197
N-(4-[4-[(4-nitrophenyl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000191
N-(4-[4-[(furan-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000487
N-(4-[4-[(furan-3-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000295
N-(4-[4-[(naphthalen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000196
N-benzyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
Homo sapiens
-
at pH 7.5 and 37°C
0.000022
N-phenyl-4-[[(pyridin-3-ylmethyl)carbamothioyl]amino]benzenesulfonamide
Homo sapiens
-
at pH 7.5 and 37°C
0.0000098
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000137
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(pyridin-4-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000388
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-2-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000225
N-[(pyridin-3-yl)methyl]-N'-(4-[4-[(thiophen-3-yl)methyl]piperazine-1-sulfonyl]phenyl)thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000369
N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethoxy)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000237
N-[(pyridin-3-yl)methyl]-N'-[4-(4-[[4-(trifluoromethyl)phenyl]methyl]piperazine-1-sulfonyl)phenyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000177
N-[(pyridin-3-yl)methyl]-N'-[4-[4-(pyridin-2-yl)piperazine-1-sulfonyl]phenyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.149
N-[2-(3,4-dimethoxyphenyl)ethyl]-1-benzothiophene-2-carboxamide
Homo sapiens
-
at pH 7.5 and 37°C
0.0000405
N-[4-(4-acetylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000009
N-[4-(4-benzylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000142
N-[4-(4-cyclohexylpiperazine-1-sulfonyl)phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
6.443
N-[4-[(4E)-4-(2,3-dimethoxybenzylidene)-5-oxo-4,5-dihydro-1,3-oxazol-2-yl]phenyl]thiophene-2-carboxamide
Homo sapiens
-
at pH 7.5 and 37°C
0.0000154
N-[4-[4-(4-methylphenyl)piperazine-1-sulfonyl]phenyl]-N'-[(pyridin-3-yl)methyl]thiourea
Homo sapiens
-
at pH 7.5 and 37°C
0.0000217
tert-butyl 4-[4-([[(pyridin-3-yl)methyl]carbamothioyl]amino)benzene-1-sulfonyl]piperazine-1-carboxylate
Homo sapiens
-
at pH 7.5 and 37°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.00213
-
at 0.001 mM 5-phosphoribosyl 1-diphosphate, without ATP, pH 7.5, 37°C
0.0259
0.0393
-
substrate nicotinamide, without ATP, pH 7.5, 37°C
0.0397
-
substrate nicotinamide, with 1 mM ATP, pH 7.5, 37°C
0.0481
-
at 0.050 mM 5-phosphoribosyl 1-diphosphate, with 1 mM ATP, pH 7.5, 37°C
0.0704
-
at 0.001 mM 5-phosphoribosyl 1-diphosphate, with 1 mM ATP, pH 7.5, 37°C
0.0741
-
substrate 5-phosphoribosyl 1-diphosphate, with 1 mM ATP, pH 7.5, 37°C
additional information
-
activity per g hemoglobin
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
for both, NMN synthesis and ATP hydrolysis activity
6.8 - 7.6
-
-
8.8
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5 - 8.5
preincubation of NAMPT for 1 h at 25 °C and various pH values in presence of 1 microM nicotinamide, 1 mM ATP, 30 nM NAMPT (NAMPT reaction started with 200 microM alpha-D-5-phosphoribosyl 1-diphosphate) or 2 mM ATP, 0.75 microM NAMPT (ATP hydrolysis)
6.1 - 8.5
-
about half-maximal activity at pH 6.1 and pH 8.5
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
35
-
assay at
37
-
assay at
pI VALUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.69
theoretic value
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
from blood from healthy individuals
Manually annotated by BRENDA team
PBMC from blood from healthy individuals
Manually annotated by BRENDA team
from individual with Hutchison-Gilford progeria syndrome associated with premature atherosclerosis, cell lifespan extension upon Nampt overexpression
Manually annotated by BRENDA team
-
diploid, GM 1362, from patient with Lesch-Nyhan disease
Manually annotated by BRENDA team
-
release of NAMPT enzyme into the cell culture supernatant occurs constitutively. In primary hepatocytes, secretion within 24 h is far higher than the cellular content, but is neither influenced by inhibitors of secretion nor by glucose, insulin or TNFalpha. In primary human hepatocytes, secreted NAMPT is less active than intracellular enzyme
Manually annotated by BRENDA team
-
leukemia cell line
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
physiological function
physiological function
-
required for de novo lipogenesis in tumor cells
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
NAMPT_HUMAN
491
0
55521
Swiss-Prot
other Location (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
55520
2 * 55520, theoretic value
120000
-
gel filtration, most of the enzyme in supernatant of HepG2 cells
52000
-
x * 52000, immunoblot analysis
55000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
according to sedimentation-equilibrium measurements following ultracentrifugation of the protein solution
homodimer
dimer
-
2 * 55000, SDS-PAGE, plus some monomer, supernatant of HepG2 cells
monomer
-
1 * 55000, SDS-PAGE, plus some dimer, supernatant of HepG2 cells
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
apo enzyme, diffraction of third crystals at 2 A resolution at -174°C, crystals belong to space group P2(1) with unit-cell parameters a = 60.56 A, b = 106.40 A, c =82.78 A, beta = 96.50°, technique: 1 microlitre of 10 mg/ml protein solution to 1 microlitre reservoir solution (38% pentaerytritol propoxylate (5/4 PO/OH) and 200 mM KCl pH 9) one week at 4°C, generation of first crystals by hanging-drop vapour diffusion (Index HT screening kit), generation of second crystals by microseeding: reservoir solution contained crushed first crystals, generation of third crystals by Repeated Seeding Technique: reservoir solution contained crushed second crystals
crystal structures at up to 2.1 A resolution of NMPRTase, alone and in complex with the reaction product nicotinamide mononucleotide or the inhibitor FK866. Crystals of the selenomethionyl free enzyme of human NMPRTase (F132M I151M double mutant) are grown with the sitting drop vapor diffusion method at 22°C. Crystals of wild-type human NMPRTase in complex with NMN are obtained at 22°C by sitting drop vapor diffusion
crystal structures of the enzyme in the free form and bound to nicotinamide and 5-phospho-alpha-D-ribose 1-diphosphate at the resolution of 2.0 A to 2.2 A are essentially identical to that of the complex with nicotinamide mononucleotide, except for some variations that can facilitate the substitution reaction by fixing the nucleophile and the leaving group for the requisite inversion of configuration at the C1’-carbon of the ribose ring. In the active site near the C1’-atom of the bound 5-phospho-alpha-D-ribose 1-diphosphate or nicotinamide mononucleotide, there is neither negatively charged group nor waterproof environment necessary to support the feasibility of a ribo-oxocarbocation intermediate inherent in the SN1 mechanism
crystallization of recombinant human NMPRTase in the free form, sitting-drop vapour-diffusion method, hanging-drop vapour-diffusion method, crystal quality is improved by successive use of the microseeding technique. The resultant crystals diffract to 2.0 A resolution. These crystals belongs to space group P2(1), with unit-cell parameters a = 60.56, b = 106.40, c = 82.78 A
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A244M
the mutation prevents inhibitor binding
D219A
inactive
D219S
the mutation leads to a switch in substrate affinity
D313A
inactive
DELTA D93
naturally occuring mutation in CHS-828 or APO866 resistant cell lines, about 20% of wild type aczivity
G217R
the mutation prevents inhibitor binding
G384A
inactive
H191R
H191R/K342R
naturally occuring mutation in APO866 resistant cell line
H191R/K342R/Q388R
naturally occuring mutation in TP201565 resistant cell line
H247A
H247E
K342R
Q388R
the mutation prevents dimerization
R311A
inactive
R311D
the inactive mutant retains the same ability as wild type enzyme in STAT-3 activation, interleukin-6 secretion, macrophage survival following endoplasmic reticulum stress, and M2-polarization
R392A
the inactive mutant retains the same ability as wild type enzyme in STAT-3 activation, interleukin-6 secretion, macrophage survival following endoplasmic reticulum stress, and M2-polarization
S199D
the mutation prevents dimerization and leads to loss of activity
S200D
the mutant retains the same ability as wild type enzyme in STAT-3 activation, interleukin-6 secretion, macrophage survival following endoplasmic reticulum stress, and M2-polarization. The mutation prevents dimerization
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5 - 8.5
preincubation of 30 nM NAMPT for 1 h at 25 °C and various pH values, NMN synthesis: reaction started with 200 microM alpha-D-5-phosphoribosyl 1-diphosphate in presence of 1 microM nicotinamide, 1 mM ATP
690900
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
65
-
10 min, stable, heat treatment during purification
70
-
5 min, stable, heat treatment during purification
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
freeze-thawing inactivates
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-70°C, in crude erythrocyte lysates, at least 30 days
-
-80°C, crude, 4-6 months
-
4°C, crude, inactivation overnight
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
immobilized metal ion affinity chromatography (Ni2+)
lysis of bacteria by French press, elution from Ni-NTA column by 100 and 200 mM imidazole, concentration and desalting, elution from HiLoad Superdex 200GP 26/60 column with 100 mM HEPES pH 7.5, 100 mM NaCl, 10 mM beta-mercaptoethanol, concentrated to 50-75 mg/ml, kept frozen
lysis of bacteria by ultrasonification in presence of 1 mM phenylmethylsulfonylfluorid (PMSF) and 1 mM dithiothreitol (DTT), ultracentrifugation, supernatant applied to glutathione Sepharose 4B beads and washed, cleavage of glutathione S-transferase (GST) tag by PreScission Protease, purification by gel-filtration chromatography in Tris-HCl pH 8.5, 150 mM NaCl, 1 mM DTT, concentration to 10 mg/ml by ultrafiltration on Microcon YM-10, stored at 4°C
Ni-NTA resin column chromatography
partial
-
partially frim K-562 leukemic cells
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
cDNA into pGEX6p1 for expression in Escherichia coli BL21 (DE) as glutathione S-transferase (GST) tagged fusion protein
chemically synthesised DNA (DNA 2.0) in pBAD DEST 49 for expression in Escherichia coli BL21 (DE3)-pLys
expressed in Escherichia coli BL21(DE3) cells
expressed in Escherichia coli Rosetta 2 (DE3)
expressed in Mus musculus
expression in Escherichia coli
expression in Escherichia coli BL21
in pQCXIP-IHRES-PURO for retroviral delivery and stable overexpression in Phoenix-amphotropic retrovirus packaging cell line
a retroviral gene delivery system is used to generate human cells stably overexpressing Nampt. Introducing the Nampt gene into aging human SMCs delays senescence and substantially lengthened cell lifespan, together with enhanced resistance to oxidative stress
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
enzyme expression is decreased by insulin, PI3K and AKT inhibitors, quercetin
enzyme expression is increased by Ox-LDL, CTRP3, glucose, rosiglitazone, adipocyte differentiation, ATP, LPS, CoCl2, ischaemia, OGD, anti-CD38 and differentiation in CCL, oxidative stress (H2O2), hypoxia, TNF-alpha, interleukin-1beta, starvation, and C-peptide
miR410 directly inhibits enzyme expression
the enzyme is often overexpressed in tumor tissues, including in breast, gastric, pancreatic, colorectal, ovarian, prostate, thyroid and endometrial carcinomas as well as in brain tumors, sarcoma, melanoma and hematological malignancies
increased during macrophage differentiation
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
inhibitor-soaking experiments
medicine
pharmacology
NAMPT inhibition might have therapeutic efficacy in immune-mediated inflammatory diseases through impact on inflammatory cytokine secretion by leukocytes
medicine
-
a dose of 75 mg/kg GMX1777, i.e. 1-[2-(2-(2-(2-methoxyethoxy)-ethoxy)ethoxy)-ethoxy-carbonyloxymethyl]-4-[N'-cyano-N''-(6-(4-chlorophenyl)-hexyl)-N-guanidino]pyridinium chloride, prodrug of GMX1778, administered over a 24 h intravenous infusion causes tumor regression in the IM-9 model, the SHP-77 model, and HCT-116 model. A 72 h continuous intravenous infusion is also effective in the IM-9 model, but is associated with smaller therapeutic index
pharmacology
-
enzyme is a potential target for development of anticancer drugs
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Preiss, J.; Handler, P.
Enzymatic synthesis of nicotinamide mononucleotide
J. Biol. Chem.
225
759-770
1957
Homo sapiens
Manually annotated by BRENDA team
Elliott, G.C.; Rechsteiner, M.C.
Evidence for a physiologically active nicotinamide phosphoribosyltransferase in cultured human fibroblasts
Biochem. Biophys. Res. Commun.
104
996-1002
1982
Homo sapiens
Manually annotated by BRENDA team
Rocchigiani, M.; Micheli, V.; Duley, J.A.; Simmonds, H.A.
Determination of nicotinamide phosphoribosyltransferase activity in human erythrocytes: high-performance liquid chromatography-linked method
Anal. Biochem.
205
334-336
1992
Homo sapiens
Manually annotated by BRENDA team
Hasmann, M.; Schemainda, I.
FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis
Cancer Res.
63
7436-7442
2003
Homo sapiens
Manually annotated by BRENDA team
Takahashi, R.; Nakamura, S.; Yoshida, T.; Kobayashi, Y.; Ohkubo, T.
Crystallization of human nicotinamide phosphoribosyltransferase
Acta Crystallogr. Sect. F
F63
375-377
2007
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
van der Veer, E.; Ho, C.; ONeil, C.; Barbosa, N.; Scott, R.; Cregan, S.P.; Pickering, J.G.
Extension of human cell lifespan by nicotinamide phosphoribosyltransferase
J. Biol. Chem.
282
10841-10845
2007
Homo sapiens, Homo sapiens (P43490)
Manually annotated by BRENDA team
Khan, J.A.; Tao, X.; Tong, L.
Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents
Nat. Struct. Mol. Biol.
13
582-588
2006
Homo sapiens (P43490), Homo sapiens, Mus musculus (Q99KQ4), Mus musculus
Manually annotated by BRENDA team
Takahashi, R.; Nakamura, S.; Yoshida, T.; Kobayashi, Y.; Ohkubo, T.
Crystallization of human nicotinamide phosphoribosyltransferase
Acta Crystallogr. Sect. F
63
375-377
2007
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Burgos, E.S.; Schramm, V.L.
Weak Coupling of ATP Hydrolysis to the Chemical Equilibrium of Human Nicotinamide Phosphoribosyltransferase
Biochemistry
47
11086-11096
2008
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Busso, N.; Karababa, M.; Nobile, M.; Rolaz, A.; Van Gool, F.; Galli, M.; Leo, O.; So, A.; De Smedt, T.
Pharmacological inhibition of nicotinamide phosphoribosyltransferase/visfatin enzymatic activity identifies a new inflammatory pathway linked to NAD
PLoS ONE
3
e2267
2008
Homo sapiens (P43490), Mus musculus (Q99KQ4)
Manually annotated by BRENDA team
Beauparlant, P.; Bedard, D.; Bernier, C.; Chan, H.; Gilbert, K.; Goulet, D.; Gratton, M.O.; Lavoie, M.; Roulston, A.; Turcotte, E.; Watson, M.
Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777
Anticancer Drugs
20
346-354
2009
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Garten, A.; Petzold, S.; Barnikol-Oettler, A.; Koerner, A.; Thasler, W.E.; Kratzsch, J.; Kiess, W.; Gebhardt, R.
Nicotinamide phosphoribosyltransferase (NAMPT/PBEF/visfatin) is constitutively released from human hepatocytes
Biochem. Biophys. Res. Commun.
391
376-381
2010
Homo sapiens
Manually annotated by BRENDA team
Takahashi, R.; Nakamura, S.; Nakazawa, T.; Minoura, K.; Yoshida, T.; Nishi, Y.; Kobayashi, Y.; Ohkubo, T.
Structure and reaction mechanism of human nicotinamide phosphoribosyltransferase
J. Biochem.
147
95-107
2010
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Colombano, G.; Travelli, C.; Galli, U.; Caldarelli, A.; Chini, M.G.; Canonico, P.L.; Sorba, G.; Bifulco, G.; Tron, G.C.; Genazzani, A.A.
A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry
J. Med. Chem.
53
616-623
2010
Homo sapiens (P43490)
Manually annotated by BRENDA team
Olesen, U.; Petersen, J.; Garten, A.; Kiess, W.; Yoshino, J.; Imai, S.; Christensen, M.; Fristrup, P.; Thougaard, A.; Bjrkling, F.; Jensen, P.; Nielsen, S.; Sehested, M.
Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase
BMC Cancer
10
677
2010
Homo sapiens (P43490)
Manually annotated by BRENDA team
Friebe, D.; Neef, M.; Kratzsch, J.; Erbs, S.; Dittrich, K.; Garten, A.; Petzold-Quinque, S.; Blueher, S.; Reinehr, T.; Stumvoll, M.; Blueher, M.; Kiess, W.; Koerner, A.
Leucocytes are a major source of circulating nicotinamide phosphoribosyltransferase (NAMPT)/pre-B cell colony (PBEF)/visfatin linking obesity and inflammation in humans
Diabetologia
54
1200-1211
2011
Homo sapiens
Manually annotated by BRENDA team
Dahl, T.; Ranheim, T.; Holm, S.; Berge, R.; Aukrust, P.; Halvorsen, B.
Nicotinamide phosphoribosyltransferase and lipid accumulation in macrophages
Eur. J. Clin. Invest.
41
1098-1104
2011
Homo sapiens
Manually annotated by BRENDA team
Zhang, L.Q.; Heruth, D.P.; Ye, S.Q.
Nicotinamide phosphoribosyltransferase in human diseases
J. Bioanal. Biomed.
3
13-25
2011
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Pittelli, M.; Formentini, L.; Faraco, G.; Lapucci, A.; Rapizzi, E.; Cialdai, F.; Romano, G.; Moneti, G.; Moroni, F.; Chiarugi, A.
Inhibition of nicotinamide phosphoribosyltransferase: cellular bioenergetics reveals a mitochondrial insensitive NAD pool
J. Biol. Chem.
285
34106-34114
2010
Homo sapiens
Manually annotated by BRENDA team
Zhang, H.S.; Sang, W.W.; Wang, Y.O.; Liu, W.
Nicotinamide phosphoribosyltransferase/sirtuin 1 pathway is involved in human immunodeficiency virus type 1 Tat-mediated long terminal repeat transactivation
J. Cell. Biochem.
110
1464-1470
2010
Homo sapiens
Manually annotated by BRENDA team
Hara, N.; Yamada, K.; Shibata, T.; Osago, H.; Tsuchiya, M.
Nicotinamide phosphoribosyltransferase/visfatin does not catalyze nicotinamide mononucleotide formation in blood plasma
PLoS ONE
6
e22781
2011
Homo sapiens
Manually annotated by BRENDA team
Bowlby, S.C.; Thomas, M.J.; D'Agostino, R.B.; Kridel, S.J.
Nicotinamide phosphoribosyl transferase (Nampt) is required for de novo lipogenesis in tumor cells
PLoS ONE
7
e40195
2012
Homo sapiens
Manually annotated by BRENDA team
Zheng, X.; Bair, K.W.; Bauer, P.; Baumeister, T.; Bowman, K.K.; Buckmelter, A.J.; Caligiuri, M.; Clodfelter, K.H.; Feng, Y.; Han, B.; Ho, Y.C.; Kley, N.; Li, H.; Liang, X.; Liederer, B.M.; Lin, J.; Ly, J.; OBrien, T.; Oeh, J.; Oh, A.; Reynolds, D.J.; Sampath, D.; Sharma, G.; Skelton, N.; Smith, C.C.; Tremayne, J.
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)
Bioorg. Med. Chem. Lett.
23
5488-5497
2013
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
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
Bioorg. Med. Chem. Lett.
24
337-343
2014
Homo sapiens (P43490)
Manually annotated by BRENDA team
Clark, D.E.; Waszkowycz, B.; Wong, M.; Lockey, P.M.; Adalbert, R.; Gilley, J.; Clark, J.; Coleman, M.P.
Application of virtual screening to the discovery of novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with potential for the treatment of cancer and axonopathies
Bioorg. Med. Chem. Lett.
26
2920-2926
2016
Homo sapiens (P43490)
Manually annotated by BRENDA team
Chen, W.; Dong, G.; He, S.; Xu, T.; Wang, X.; Liu, N.; Zhang, W.; Miao, C.; Sheng, C.
Identification of benzothiophene amides as potent inhibitors of human nicotinamide phosphoribosyltransferase
Bioorg. Med. Chem. Lett.
26
765-768
2016
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Grolla, A.A.; Travelli, C.; Genazzani, A.A.; Sethi, J.K.
Extracellular nicotinamide phosphoribosyltransferase, a new cancer metabokine
Br. J. Pharmacol.
173
2182-2194
2016
Homo sapiens (P43490)
Manually annotated by BRENDA team
Hsu, C.P.; Yamamoto, T.; Oka, S.; Sadoshima, J.
The function of nicotinamide phosphoribosyltransferase in the heart
DNA Repair
23
64-68
2014
Homo sapiens (P43490)
Manually annotated by BRENDA team
Marletta, A.S.; Massarotti, A.; Orsomando, G.; Magni, G.; Rizzi, M.; Garavaglia, S.
Crystal structure of human nicotinic acid phosphoribosyltransferase
FEBS Open Bio
5
419-428
2015
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Pittelli, M.; Cavone, L.; Lapucci, A.; Oteri, C.; Felici, R.; Niccolai, E.; Amedei, A.; Chiarugi, A.
Nicotinamide phosphoribosyltransferase (NAMPT) activity is essential for survival of resting lymphocytes
Immunol. Cell Biol.
92
191-199
2014
Mus musculus, Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Tan, B.; Young, D.; Lu, Z.; Wang, T.; Meier, T.; Shepard, R.; Roth, K.; Zhai, Y.; Huss, K.; Kuo, M.; Gillig, J.; Parthasarathy, S.; Burkholder, T.; Smith, M.; Geeganage, S.; Zhao, G.
Pharmacological inhibition of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme essential for NAD+ biosynthesis, in human cancer cells: Metabolic basis and potential clinical implications
J. Biol. Chem.
288
3500-3511
2013
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
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
J. Med. Chem.
56
6413-6433
2013
Homo sapiens (P43490)
Manually annotated by BRENDA team
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
Sci. Rep.
5
10043
2015
Homo sapiens
Manually annotated by BRENDA team
Zabka, T.S.; Singh, J.; Dhawan, P.; Liederer, B.M.; Oeh, J.; Kauss, M.A.; Xiao, Y.; Zak, M.; Lin, T.; McCray, B.; La, N.; Nguyen, T.; Beyer, J.; Farman, C.; Uppal, H.; Dragovich, P.S.; OBrien, T.; Sampath, D.; Misner, D.L.
Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase
Toxicol. Sci.
144
163-172
2015
Homo sapiens (P43490), Homo sapiens, Rattus norvegicus (Q80Z29)
Manually annotated by BRENDA team
Oita, R.C.; Camp, S.M.; Ma, W.; Ceco, E.; Harbeck, M.; Singleton, P.; Messana, J.; Sun, X.; Wang, T.; Garcia, J.G.N.
Novel mechanism for nicotinamide phosphoribosyltransferase inhibition of TNF-alpha-mediated apoptosis in human lung endothelial cells
Am. J. Respir. Cell Mol. Biol.
59
36-44
2018
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Asawa, Y.; Katsuragi, K.; Sato, A.; Yoshimori, A.; Tanuma, S.I.; Nakamura, H.
Structure-based drug design of novel carborane-containing nicotinamide phosphoribosyltransferase inhibitors
Bioorg. Med. Chem.
27
2832-2844
2019
Homo sapiens (P43490)
Manually annotated by BRENDA team
Curtin, M.L.; Heyman, H.R.; Clark, R.F.; Sorensen, B.K.; Doherty, G.A.; Hansen, T.M.; Frey, R.R.; Sarris, K.A.; Aguirre, A.L.; Shrestha, A.; Tu, N.; Woller, K.; Pliushchev, M.A.; Sweis, R.F.; Cheng, M.; Wilsbacher, J.L.; Kovar, P.J.; Guo, J.; Cheng, D.; Longenecker, K.L.; Raich, D.; Korepanova, A.V.; Soni, N.B.; Algire, M.A.
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT)
Bioorg. Med. Chem. Lett.
27
3317-3325
2017
Homo sapiens (P43490)
Manually annotated by BRENDA team
Zhang, K.; Ni, Y.; Chen, J.; Tu, Z.; Wu, X.; Chen, D.; Yao, H.; Jiang, S.
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer
Bioorg. Med. Chem. Lett.
29
1502-1506
2019
Homo sapiens (P43490)
Manually annotated by BRENDA team
Torretta, S.; Colombo, G.; Travelli, C.; Boumya, S.; Lim, D.; Genazzani, A.A.; Grolla, A.A.
The cytokine nicotinamide phosphoribosyltransferase (eNAMPT; PBEF; visfatin) acts as a natural antagonist of C-C chemokine receptor type 5 (CCR5)
Cells
9
496
2020
Homo sapiens (P43490), Mus musculus (Q99KQ4)
Manually annotated by BRENDA team
Aprile, S.; Galli, U.; Tron, G.C.; Del Grosso, E.; Travelli, C.; Grosa, G.
Data on metabolic stability, aqueous solubility and CYP inhibition of novel triazole-based nicotinamide phosphoribosyltransferase (NAMPT) inhibitors
Data Brief
28
105034
2020
Homo sapiens (P43490)
Manually annotated by BRENDA team
Travelli, C.; Aprile, S.; Mattoteia, D.; Colombo, G.; Clemente, N.; Scanziani, E.; Terrazzino, S.; Alisi, M.A.; Polenzani, L.; Grosa, G.; Genazzani, A.A.; Tron, G.C.; Galli, U.
Identification of potent triazolylpyridine nicotinamide phosphoribosyltransferase (NAMPT) inhibitors bearing a 1,2,3-triazole tail group
Eur. J. Med. Chem.
181
111576
2019
Homo sapiens (P43490)
Manually annotated by BRENDA team
Svoboda, P.; Krizova, E.; Sestakova, S.; Vapenkova, K.; Knejzlik, Z.; Rimpelova, S.; Rayova, D.; Volfova, N.; Krizova, I.; Rumlova, M.; Sykora, D.; Kizek, R.; Haluzik, M.; Zidek, V.; Zidkova, J.; Skop, V.
Nuclear transport of nicotinamide phosphoribosyltransferase is cell cycle-dependent in mammalian cells, and its inhibition slows cell growth
J. Biol. Chem.
294
8676-8689
2019
Homo sapiens (P43490), Mus musculus (Q99KQ4)
Manually annotated by BRENDA team
Szefler, B.; Czelen, P.
Potential inhibitory effect of indolizine derivatives on the two enzymes nicotinamide phosphoribosyltransferase and beta lactamase, a molecular dynamics study
J. Mol. Model.
23
208
2017
Homo sapiens (P43490)
Manually annotated by BRENDA team
Hara, N.; Osago, H.; Hiyoshi, M.; Kobayashi-Miura, M.; Tsuchiya, M.
Quantitative analysis of the effects of nicotinamide phosphoribosyltransferase induction on the rates of NAD+ synthesis and breakdown in mammalian cells using stable isotope-labeling combined with mass spectrometry
PLoS ONE
14
e0214000
2019
Homo sapiens (P43490), Rattus norvegicus (Q80Z29), Mus musculus (Q99KQ4)
Manually annotated by BRENDA team
Gao, H.; Chen, J.; Chen, T.; Wang, Y.; Song, Y.; Dong, Y.; Zhao, S.; Machado, R.F.
MicroRNA410 inhibits pulmonary vascular remodeling via regulation of nicotinamide phosphoribosyltransferase
Sci. Rep.
9
9949
2019
Homo sapiens (P43490), Homo sapiens
Manually annotated by BRENDA team
Audrito, V.; Manago, A.; Gaudino, F.; Deaglio, S.
Targeting metabolic reprogramming in metastatic melanoma The key role of nicotinamide phosphoribosyltransferase (NAMPT)
Semin. Cell Dev. Biol.
98
192-201
2020
Homo sapiens (P43490)
Manually annotated by BRENDA team