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Information on EC 3.6.1.9 - nucleotide diphosphatase and Organism(s) Homo sapiens
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3.6.1.9 nucleotide diphosphataseIUBMB Comments
The enzyme preferentially hydrolyses ATP, but can also hydrolyse other nucleoside 5' triphosphates such as GTP, CTP, TTP and UTP to their corresponding monophosphates. In vitro the enzyme also acts as a nucleotidohydrolase on ADP, NAD+, NADP+, FAD, and CoA.
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Word Map
- 3.6.1.9
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ecosystem
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climate
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forest
- accident
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basophil
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chernobyl
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terrestrial
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land
-
atmospheric
- phosphorus
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grassland
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aboveground
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fukushima
- allergy
- ribavirin
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radionuclides
- phytase
- thiopurine
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tibia
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belowground
- ash
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canopy
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budget
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boreal
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biome
- rbv
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anti-ige
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modis
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interannual
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meteorological
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disaster
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arid
- azathioprine
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ukraine
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hydrological
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rainfall
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corn-soybean
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coniferous
- ectonucleotidases
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peg-ifn
- ntpdases
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earthquake
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croplands
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ecto-nucleoside
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diphosphohydrolase
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year-1
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land-use
- mercaptopurine
- e-ntpdase
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steppe
- medicine
- drug development
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Synonyms
npp, cd203c, itpase, inosine triphosphatase, inosine triphosphate pyrophosphatase, maf protein, enpp3, nppase, e-npp, nucleoside triphosphate pyrophosphohydrolase, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
E-NPP
E-NPP3
ecto-nucleotide pyrophosphatase/phosphodiesterase
ectonucleotide pyrophosphatase/phosphodiesterase 1
ENPP1
NPP
NPP1
NPP2
NPP3
nucleoside triphosphate diphosphatase
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-
-
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nucleoside-triphosphate pyrophosphatase
-
-
-
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nucleotide pyrophosphatase
nucleotide pyrophosphatase/phosphodiesterase
nucleotide pyrophosphohydrolase
-
-
-
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nucleotide-sugar pyrophosphatase
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-
-
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pyrophosphatase, nucleoside triphosphate
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-
-
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nucleotide pyrophosphatase
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-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of phosphoric ester
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-
-
-
PATHWAY SOURCE
PATHWAYS
BRENDA
KEGG
-
-, -, -, -, -, -, -
SYSTEMATIC NAME
IUBMB Comments
dinucleotide nucleotidohydrolase
The enzyme preferentially hydrolyses ATP, but can also hydrolyse other nucleoside 5' triphosphates such as GTP, CTP, TTP and UTP to their corresponding monophosphates. In vitro the enzyme also acts as a nucleotidohydrolase on ADP, NAD+, NADP+, FAD, and CoA.
CAS REGISTRY NUMBER
COMMENTARY
9032-64-8
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
4-nitrophenyl phenyl phosphate + H2O
4-nitrophenol + phenyl phosphate
-
-
-
?
4-nitrophenyl-5'-adenosine monophosphate + H2O
4-nitrophenol + 5'-adenosine monophosphate
artificial substrate
-
-
?
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano + 2 H2O
?
low hydrolysis activity with the inhibitor as substrate
-
-
?
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate + 2 H2O
?
low hydrolysis activity with the inhibitor as substrate
-
-
?
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano + 2 H2O
?
low hydrolysis activity with the inhibitor as substrate
-
-
?
dITP + H2O
dIMP + diphosphate
at the optimal pH of 10.0, the recombinant enzyme hydrolyzes ITP, dITP, and xanthosine 5'-triphosphate to their respective monophosphates whereas activity with other nucleoside triphosphates is low. UTP, (d)CTP, TTP, and (d)ATP are hydrolyzed 10-100fold less than dITP. IDP and IMP are not hydrolyzed at all
-
-
?
ITP + H2O
IMP + diphosphate
at the optimal pH of 10.0, the recombinant enzyme hydrolyzes ITP, dITP, and xanthosine 5'-triphosphate to their respective monophosphates whereas activity with other nucleoside triphosphates is low. UTP, (d)CTP, TTP, and (d)ATP are hydrolyzed 10-100fold less than dITP. IDP and IMP are not hydrolyzed at all
-
-
?
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + phenylphosphonate
-
phosphodiesterase-1 activity
-
?
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate + 2 H2O
?
low hydrolysis activity with the inhibitor as substrate
-
-
?
thymidine 5'-monophosphate p-nitrophenyl ester + H2O
thymidine 5'-monophosphate + p-nitrophenol
UDP-N-acetyl-alpha-D-galactosamine + H2O
N-acetyl-alpha-D-galactosaminyl-1-phosphate + UMP
-
-
-
?
UDP-N-acetyl-alpha-D-glucosamine + H2O
UMP + N-acetyl-alpha-D-glucosaminyl-1-phosphate
-
-
-
?
xanthosine 5'-triphosphate + H2O
xanthosine 5'-monophosphate + diphosphate
at the optimal pH of 10.0, the recombinant enzyme hydrolyzes ITP, dITP, and xanthosine 5'-triphosphate to their respective monophosphates whereas activity with other nucleoside triphosphates is low. UTP, (d)CTP, TTP, and (d)ATP are hydrolyzed 10-100fold less than dITP. IDP and IMP are not hydrolyzed at all
-
-
?
3'-phosphoadenosine 5'-phosphosulfate + H2O
3'-phosphoadenosine + phosphosulfate
-
-
-
?
3'-phosphoadenosine 5'-phosphosulfate + H2O
3'-phosphoadenosine + phosphosulfate
-
-
-
?
4-nitrophenyl 5'-thymidine monophosphate + H2O
4-nitrophenol + 5'-thymidine monophosphate
-
-
-
?
4-nitrophenyl 5'-thymidine monophosphate + H2O
4-nitrophenol + 5'-thymidine monophosphate
-
-
-
?
4-nitrophenyl-5'-thymidine monophosphate + H2O
4-nitrophenol + 5'-thymidine monophosphate
-
-
-
?
4-nitrophenyl-5'-thymidine monophosphate + H2O
4-nitrophenol + 5'-thymidine monophosphate
-
-
-
?
4-nitrophenyl-5'-thymidine monophosphate + H2O
4-nitrophenol + 5'-thymidine monophosphate
artificial substrate
-
-
?
4-nitrophenyl-5'-TMP + H2O
4-nitrophenol + 5'-TMP
hydrolysis of pnp-TMP at the cell surface of both osteocarcinoma and colon cancer cells
-
-
?
4-nitrophenyl-5'-TMP + H2O
4-nitrophenol + 5'-TMP
a specific NPP substrate
-
-
?
thymidine 5'-monophosphate p-nitrophenyl ester + H2O
thymidine 5'-monophosphate + p-nitrophenol
-
-
-
?
thymidine 5'-monophosphate p-nitrophenyl ester + H2O
thymidine 5'-monophosphate + p-nitrophenol
-
-
-
?
additional information
?
-
-
E-NPP3 is associated with carcinogenesis of human colon cancer
-
-
?
additional information
?
-
NPP1 hydrolyzes a wide range of phosphodiester bonds, e.g. in nucleoside triphosphates, (cyclic) dinucleotides, and nucleotide sugars yielding nucleoside 5'-monophosphates as products. Its main substrate is ATP which is cleaved to AMP and diphosphate. Purine nucleotides (ATP and GTP) are better substrates than pyrimidine nucleotides (CTP and UTP). Besides, NPP1 metabolizes other nucleotides, e.g. nicotinamide adenine dinucleotide (NAD+), 3'-phosphoadenosine-5'-phosphosulfate (PAPS), diadenosine polyphosphates like diadenosine triphosphate (AP3A) or diadenosine tetraphosphate (AP4A), and UDP-glucose
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-
-
additional information
?
-
-
NPP1 hydrolyzes a wide range of phosphodiester bonds, e.g. in nucleoside triphosphates, (cyclic) dinucleotides, and nucleotide sugars yielding nucleoside 5'-monophosphates as products. Its main substrate is ATP which is cleaved to AMP and diphosphate. Purine nucleotides (ATP and GTP) are better substrates than pyrimidine nucleotides (CTP and UTP). Besides, NPP1 metabolizes other nucleotides, e.g. nicotinamide adenine dinucleotide (NAD+), 3'-phosphoadenosine-5'-phosphosulfate (PAPS), diadenosine polyphosphates like diadenosine triphosphate (AP3A) or diadenosine tetraphosphate (AP4A), and UDP-glucose
-
-
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
4-nitrophenyl-5'-TMP + H2O
4-nitrophenol + 5'-TMP
hydrolysis of pnp-TMP at the cell surface of both osteocarcinoma and colon cancer cells
-
-
?
UDP-N-acetyl-alpha-D-galactosamine + H2O
N-acetyl-alpha-D-galactosaminyl-1-phosphate + UMP
-
-
-
?
UDP-N-acetyl-alpha-D-glucosamine + H2O
UMP + N-acetyl-alpha-D-glucosaminyl-1-phosphate
-
-
-
?
additional information
?
-
-
E-NPP3 is associated with carcinogenesis of human colon cancer
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
Mg2+
Zn2+
Mg2+
activity increases sharply up to about 10 mM MgCl2 and reaches a plateau between about 30 and 100 mM
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2E)-2-([3-methoxy-4-[(1H-tetrazol-5-yl)methoxy]phenyl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-[(2-oxo-1,2-dihydroquinolin-3-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-[(5-iodofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
moderate to low inhibition
(2E)-2-[(naphthalen-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2E)-2-[[2,4-bis(4-methylpiperidin-1-yl)-5-nitrophenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(2E)-3-phenylprop-2-en-1-ylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(3-phenoxyphenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(4-chlorophenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(4-iodophenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(4-methylphenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-bromofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-iodofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
highly selective for NPP1 as compared to other human enzymes, i.e. NPP2, NPP3, NTPDases1-3, TNAP, and eN
(2Z)-2-[(5-methylfuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-nitrofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(5-phenylfuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(furan-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(pyridin-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[(thiophen-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[3-(benzyloxy)phenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[4-(morpholin-4-yl)phenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[5-(dimethylamino)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[5-(phenylsulfanyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
-
(4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
-
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
-
(4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
-
(E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
-
(R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
-
1-amino-4-[4-[(4-anilino-6-chloro-1,3,5-triazin-2-yl)amino]-3-sulfoanilino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid
-
12-methyl-6(3-methyl-1H-indol-1-yl)indolo[1,2-h][1,7]naphthyridine
-
2,3-dimethoxy-12-methyl-6-(3-methyl-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
2-(trifluoromethyl)-3,4,8-tri(4-(trifluoromethyl)phenyl)quinoline
-
2-[4-[(4-fluorobenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-fluorobenzene-1-sulfonate
-
2-[4-[(4-methoxybenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methoxybenzene-1-sulfonate
-
2-[4-[(4-methylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methylbenzene-1-sulfonate
38.5% inhibition
2-[4-[(4-tert-butylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-tert-butylbenzene-1-sulfonate
shows cytotoxicity against MCF-7 and HT-29 cell lines and shows less cytotoxicity on against A-549 cell
2-[4-[(cyclohexanesulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl cyclohexanesulfonate
30.0% inhibition
2-[4-[(dimethylsulfamoyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl dimethylsulfamate
43.7% inhibition
2-[4-[(ethanesulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl ethanesulfonate
35.1% inhibition
2-[4-[(methylsulfamoyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl methylsulfamate
36.0% inhibition
3,3'-[(2-chlorophenyl)methylene]bis(4-hydroxy-3,4-dihydro-2H-1-benzopyran-2-one)
-
3,9-difluoro-6-(6-fluoro-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
3-(3-bromo-4-chloro-2-(trifluoromethyl)quinolin-8-yl)benzonitrile
-
3-bromo-4-chloro-2-(trifluoromethyl)-8-(4-(trifluoromethyl)phenyl)quinoline
-
3-bromo-4-chloro-8-(2,5-dimethoxyphenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(3,5-difluorophenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(3,5-dimethylphenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-chloro-8-(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
3-bromo-4-N-butylamine-8-(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
3-fluoro-12-methyl-6-(3-methyl-1H-indol-1-yl)indolo[2,1-a]isoquinoline
-
3-fluoro-6-(1H-pyrrolo[2,3-b]pyridin-1-yl)pyrido[3',2':4,5]pyrrolo[2,1-a]isoquinoline
-
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[(quinoline-8-sulfonyl)oxy]-1-benzothiophen-2-yl)phenyl quinoline-8-sulfonate
28.7 inhibition; 42.5% inhibition
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[[4-(trifluoromethyl)benzene-1-sulfonyl]oxy]-1-benzothiophen-2-yl)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-(4-chlorobenzamido)phenyl 4-fluorobenzene-1-sulfonate
46% inhibition at 0.1 mM
4-chloro-2-(trifluoromethyl)-3,8-bis(4-(trifluoromethyl)phenyl)quinoline
-
4-chloro-3,8-bis(4-(trifluoromethoxy)phenyl)-2-(trifluoromethyl)quinoline
-
4-chloro-8-(2,5-dimethoxyphenyl)-2-(trifluoromethyl)-3-(4-(trifluoromethyl)phenyl)quinoline
-
4-chloro-8-phenyl-2-(trifluoromethyl)-3-(4-(trifluoromethyl)phenyl)quinoline
-
4-N-butylamine-3,8-bis(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
-
4-[(cycloheptanecarbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
29% inhibition at 0.1 mM; 37% inhibition at 0.1 mM
4-[(cycloheptanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(cycloheptanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
39.3% inhibition at 0.1 mM
4-[(cycloheptanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
-
4-[(cycloheptanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
-
4-[(cyclohexanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
39% inhibition at 0.1 mM+L345; 43% inhibition at 0.1 mM
4-[(cyclohexanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
-
4-[(cyclooctanecarbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
30% inhibition at 0.1 mM; 30% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
29% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
35% inhibition at 0.1 mM; 43% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
40% inhibition at 0.1 mM; 46% inhibition at 0.1 mM
4-[(cyclooctanecarbonyl)amino]phenyl benzenesulfonate
45% inhibition at 0.1 mM; 47% inhibition at 0.1 mM
4-[(cyclopentanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
-
4-[(cyclopentanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
-
4-[(naphthalene-2-carbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
49% inhibition at 0.1 mM
4-[(naphthalene-2-carbonyl)amino]phenyl benzenesulfonate
23% inhibition at 0.1 mM; 24% inhibition at 0.1 mM
4-[(quinoline-8-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
37% inhibition at 0.1 mM; 42% inhibition at 0.1 mM
5'-O-(boranyl[[hydroxy(phosphonomethyl)phosphoryl]oxy]phosphoryl)adenosine
-
5'-O-[([[dibromo(phosphono)methyl](hydroxy)phosphoryl]oxy)(hydroxy)phosphoryl]-N,N-diethyladenosine
-
6-(1H-benzo[d]imidazol-1-yl)benzo[4,5]imidazo[2,1-a]isoquinoline
-
6-(1H-pyrrolo[2,3-b]pyridin-1-yl)pyrido[3',2':4,5]pyrrolo[2,1-a]isoquinoline
-
6-(4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl)-9,10-dihydroindolo[2,1-a]isoquinolin-11(8H)-one
-
6-(5-cyano-1H-indol-1-yl)-2,3-dimethoxyindolo[2,1,-a]isoquinoline-10-carbonitrile
-
6-(5-cyano-1H-indol-1-yl)-3-fluoroindolo[2,1-a]isoquinoline-10-carbonitrile
-
6-(5-cyano-1H-indol-1-yl)indolo[2,1-a]isoquinoline-10-carbonitrile
-
8,8'-[carbonylbis[azanediyl-3,1-phenylenecarbonylazanediyl(4-methyl-3,1-phenylene)carbonylazanediyl]]di(naphthalene-1,3,5-trisulfonic acid)
-
8-phenyl-2-(trifluoromethyl)-3,4-bis(4-(trifluoromethyl)phenyl)quinoline
-
8-phenyl-4-(p-tolyl)-2-(trifluoromethyl)-3-(4-(trifluoromethyl)phenyl)quinoline
-
9-fluoro-6-(6-fluoro-1H-indol-1-yl)-2,3-dimethoxyindolo[2,1-a]isoquinoline
-
9-fluoro-6-(6-fluoro-1H-indol-1-yl)-[1,3]dioxolo[4,5-g]indolo[2,1-a]isoquinoline
-
Cibacron blue
-
0.1 mM, substrate Ap4A, strong inhibition, NPP1; 0.1 mM, substrate Ap4A, strong inhibition, NPP2
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate
-
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
gamma-S-adenosine 5'-(alpha,beta-methylene)triphosphate
competitive inhibition
N-(3,4-dimethoxyphenyl)-2-[(5-methoxy-3H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]acetamide
-
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl] sulfuric diamide
i.e. SAR 03004
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate
-
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid
-
0.1 mM, substrate p4A, 42% inhibition, NPP2; 0.1 mM, substrate p4A, about 85% inhibition, NPP1
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
suramin
-
0.1 mM, substrate Ap4A, about 77% inhibition, NPP2; 0.1 mM, substrate p4A, about 70% inhibition, NPP1
additional information
-
diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview
-
additional information
diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview
-
additional information
diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview
-
additional information
structure-activity relationships of thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives as selective nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitors. Inhibition mechanism, overview
-
additional information
structure-activity relationships of thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives as selective nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitors. Inhibition mechanism, overview
-
additional information
-
structure-activity relationships of thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives as selective nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitors. Inhibition mechanism, overview
-
additional information
synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview; synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview
-
additional information
synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview; synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors, structure-activity relationships, molecular docking study and analysis, overview
-
additional information
design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3; design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3
-
additional information
design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3; design and synthesis of arylated 2-trifluoromethylquinolines derivatives by site-selective, chemo-selective amination reactions following regioselective Suzuki-Miyaura coupling reactions. Evaluation of their potential to inhibit two families of ecto-nucleotidases, i.e. NPPs (EC 3.6.1.9) and nucleoside triphosphate diphosphohydrolases (NTPDases, EC 3.6.1.15), docking studies to analyze the active binding site of the molecules, overview. The compounds all show negligible inhibition of NTPDases1-3
-
additional information
synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay; synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay
-
additional information
synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay; synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile, structure activity and structure selectivity relationship of 2-benzoyl-5-methyl-1H-pyrazol-3(2H)-one derivatives, overview. The cytotoxic potential of the synthesized pyrazole derivatives is scrutinized against three different cancer cell lines i.e. breast cancer cells (MCF-7), cervical cancer cells (HeLa), and bone marrow lymphoblast cells (K-562). The assay is performed by using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide)-based cell viability assay
-
additional information
a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts, inhibition values in percent per 0.01 mM. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity; a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity
-
additional information
a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts, inhibition values in percent per 0.01 mM. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity; a series of raloxifene sulfonate/sulfamate derivatives are designed, synthesized, and tested for inhibitory effect against nucleotide pyrophosphatase/phosphodiesterase-1 and -3 (NPP1 and NPP3) enzymes. The compounds are subjected to cytotoxic studies on various cancer cell lines, and the most potent derivatives are explored for their potency against these cancer cell lines, e.g. HT-29 cells, as well as F180 fibroblasts. Structure-activity relationships, molecular modeling of inhibitor binding, overview. Pi-Pi stacking interactions and metal interactions with zinc inside the active site are noticed and contributed towards the inhibitory activity
-
additional information
synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-1, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines; synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-3, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines
-
additional information
synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-1, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines; synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-3, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines
-
additional information
-
synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-1, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines; synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation, potent inhibition of nucleotide pyrophosphatase-3, docking study, overview. Various N-fused isoquinoline derivatives are synthesized using a one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing heterocycles followed by intramolecular palladium-catalyzed C-H arylation. The method described gives convenient access to diverse structures of N-fused polycyclic isoquinolines
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0326
2',3''-cGAMP
pH and temperature not specified in the publication, soluble enzyme
0.12
3'-phosphoadenosine-5'-phosphosulfate
pH and temperature not specified in the publication, membrane enzyme
0.188
4-nitrophenyl-5'-adenosine monophosphate
pH and temperature not specified in the publication, soluble enzyme
0.222
4-nitrophenyl-5'-thymidine monophosphate
pH and temperature not specified in the publication, soluble enzyme
0.0205
Ap4A
pH and temperature not specified in the publication, soluble enzyme
0.114
cAMP
pH and temperature not specified in the publication, soluble enzyme
0.33
NAD+
pH and temperature not specified in the publication, membrane enzyme
0.0566
UTP
pH and temperature not specified in the publication, soluble enzyme
0.0051
Ap3A
pH and temperature not specified in the publication, membrane enzyme
0.0062
ATP
-
E-NPP1, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.0074
ATP
-
E-NPP3, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.00817
ATP
pH and temperature not specified in the publication, soluble enzyme
additional information
additional information
Michaelis-Menten kinetics
-
additional information
additional information
Michaelis-Menten kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
5.36
2',3''-cGAMP
pH and temperature not specified in the publication, soluble enzyme
2.51
4-nitrophenyl-5'-adenosine monophosphate
pH and temperature not specified in the publication, soluble enzyme
22.3
4-nitrophenyl-5'-thymidine monophosphate
pH and temperature not specified in the publication, soluble enzyme
5.65
Ap4A
pH and temperature not specified in the publication, soluble enzyme
5.51
ATP
pH and temperature not specified in the publication, soluble enzyme
2.16
cAMP
pH and temperature not specified in the publication, soluble enzyme
1.96
UTP
pH and temperature not specified in the publication, soluble enzyme
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
164.4
2',3''-cGAMP
pH and temperature not specified in the publication, soluble enzyme
13.35
4-nitrophenyl-5'-adenosine monophosphate
pH and temperature not specified in the publication, soluble enzyme
100.45
4-nitrophenyl-5'-thymidine monophosphate
pH and temperature not specified in the publication, soluble enzyme
275.6
Ap4A
pH and temperature not specified in the publication, soluble enzyme
674.4
ATP
pH and temperature not specified in the publication, soluble enzyme
18.95
cAMP
pH and temperature not specified in the publication, soluble enzyme
34.6
UTP
pH and temperature not specified in the publication, soluble enzyme
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.01
(2E)-2-([3-methoxy-4-[(1H-tetrazol-5-yl)methoxy]phenyl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2E)-2-benzylidene[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2E)-2-[(2-oxo-1,2-dihydroquinolin-3-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2E)-2-[(naphthalen-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.00856
(2E)-2-[[2,4-bis(4-methylpiperidin-1-yl)-5-nitrophenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.01
(2Z)-2-benzylidene[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-ethylidene[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(2E)-3-phenylprop-2-en-1-ylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(3-phenoxyphenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(4-chlorophenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(4-iodophenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(4-methylphenyl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.00061
(2Z)-2-[(5-bromofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.000467
(2Z)-2-[(5-iodofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.00211
(2Z)-2-[(5-methylfuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.00107
(2Z)-2-[(5-nitrofuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(5-phenylfuran-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.000981
(2Z)-2-[(furan-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(pyridin-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[(thiophen-2-yl)methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[[3-(benzyloxy)phenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.00891
(2Z)-2-[[4-(morpholin-4-yl)phenyl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.00421
(2Z)-2-[[5-(dimethylamino)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
pH 9.0, 37°C, NPP1
0.01
(2Z)-2-[[5-(phenylsulfanyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
above, pH 9.0, 37°C, NPP1
0.00052
1-amino-4-[4-[(4-anilino-6-chloro-1,3,5-triazin-2-yl)amino]-3-sulfoanilino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid
versus ATP, pH 9.0, 37°C, NPP1
0.01
1-[(4-methoxyphenyl)methyl]-1H-benzimidazole
above, pH 9.0, 37°C, NPP1
0.05
3,3'-[(2-chlorophenyl)methylene]bis(4-hydroxy-3,4-dihydro-2H-1-benzopyran-2-one)
versus p-nitrophenyl phenyl phosphate, pH 9.0, 37°C, NPP1
0.0005
5'-O-(boranyl[[hydroxy(phosphonomethyl)phosphoryl]oxy]phosphoryl)adenosine
versus 4-nitrophenyl 5'-thymidine monophosphate, pH 9.0, 37°C, NPP1
0.012
5'-O-[([[dibromo(phosphono)methyl](hydroxy)phosphoryl]oxy)(hydroxy)phosphoryl]-N,N-diethyladenosine
versus 4-nitrophenyl 5'-thymidine monophosphate, pH 9.0, 37°C, NPP1
0.15
5,5'-(propane-1,3-diyl)di(1,3,4-oxadiazole-2(3H)-thione)
versus p-nitrophenyl phenyl phosphate, pH 9.0, 37°C, NPP1
0.00026
8,8'-[carbonylbis[azanediyl-3,1-phenylenecarbonylazanediyl(4-methyl-3,1-phenylene)carbonylazanediyl]]di(naphthalene-1,3,5-trisulfonic acid)
versus ATP, pH 9.0, 37°C, NPP1
0.00002
adenosine 5'-alpha,beta-methylene-gamma-thiotriphosphate
versus 4-nitrophenyl 5'-thymidine monophosphate, pH 9.0, 37°C, NPP1
0.0005 - 0.056
alpha-borano-beta,gamma-MetATP
pH and temperature not specified in the publication, membrane enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.009
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
0.051
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate
with NPP1, pH 7.3, 37°C
0.02
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
with NPP1, pH 7.3, 37°C
0.002 - 0.0045
gamma-S-adenosine 5'-(alpha,beta-methylene)triphosphate
pH and temperature not specified in the publication, membrane enzyme
0.00534
N-(3,4-dimethoxyphenyl)-2-[(5-methoxy-3H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]acetamide
versus ATP, pH 9.0, 37°C, NPP1
0.000059
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
versus 4-nitrophenyl 5'-thymidine monophosphate, pH 9.0, 37°C, NPP1
0.013
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate
with NPP1, pH 7.3, 37°C
0.000005
polyoxymetalate PSB-POM141
versus 4-nitrophenyl 5'-thymidine monophosphate, pH 9.0, 37°C, NPP1
-
0.00218
2-MeSADP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.0237 - 0.0328
2-MeSADP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.0354
2-MeSADP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-adenosine monophosphate
0.00447
2-MeSATP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.0213 - 0.0253
2-MeSATP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.0399
2-MeSATP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-adenosine monophosphate
0.00128
alpha,beta-metADP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.0165
alpha,beta-metADP
pH and temperature not specified in the publication, membrane enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.0165 - 0.0243
alpha,beta-metADP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.00332
alpha,beta-metATP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.00819
alpha,beta-metATP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-adenosine monophosphate
0.013 - 0.0269
alpha,beta-metATP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.00296
benzoyl-ATP
pH and temperature not specified in the publication, membrane enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.0146
benzoyl-ATP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.009
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
with NPP1, pH 7.3, 37°C
0.009
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
versus 4-nitrophenyl 5'-thymidine monophosphate, pH 9.0, 37°C, NPP1
0.00342
dialADP
pH and temperature not specified in the publication, membrane enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.00503
dialADP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.00509
dialADP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-adenosine monophosphate
0.00514 - 0.00562
dialADP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.00409
dialATP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-thymidine monophosphate
0.00508
dialATP
pH and temperature not specified in the publication, soluble enzyme, versus 4-nitrophenyl-5'-adenosine monophosphate
0.00682 - 0.00696
dialATP
pH and temperature not specified in the publication, soluble enzyme, versus ATP
0.00052
Reactive blue 2
-
E-NPP1, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.00071
Reactive blue 2
-
E-NPP3, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.00004
suramin
-
E-NPP3, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.00026
suramin
-
E-NPP1, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0124 - 0.1
(R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
0.00181 - 0.00888
2-[4-[(4-fluorobenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-fluorobenzene-1-sulfonate
0.00042 - 0.00124
2-[4-[(4-methoxybenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methoxybenzene-1-sulfonate
0.00045
2-[4-[(4-methylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00029 - 0.00071
2-[4-[(4-tert-butylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-tert-butylbenzene-1-sulfonate
0.00049
2-[4-[(cyclohexanesulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl cyclohexanesulfonate
Homo sapiens
pH 9.5, 37°C
0.00151
2-[4-[(ethanesulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl ethanesulfonate
Homo sapiens
pH 9.5, 37°C
0.00155
2-[4-[(methylsulfamoyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl methylsulfamate
Homo sapiens
pH 9.5, 37°C
0.00023 - 0.00401
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[[4-(trifluoromethyl)benzene-1-sulfonyl]oxy]-1-benzothiophen-2-yl)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
0.002897
4-(4-chlorobenzamido)phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP29
0.000431 - 0.002578
4-[(cycloheptanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
0.002267
4-[(cycloheptanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP20
0.000387 - 0.00179
4-[(cyclohexanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
0.000214
4-[(cyclooctanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP26
0.001134 - 0.003963
4-[(cyclopentanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
0.002892 - 0.003429
4-[(naphthalene-2-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
0.001118 - 0.005426
4-[(naphthalene-2-carbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
0.002195
4-[(naphthalene-2-carbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP33
0.013
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
Homo sapiens
with NPP1, pH 7.3, 37°C
0.05
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate
Homo sapiens
with NPP1, pH 7.3, 37°C
0.063
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
Homo sapiens
with NPP1, pH 7.3, 37°C
0.033
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate
Homo sapiens
with NPP1, pH 7.3, 37°C
0.00322
(3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00181
(3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00342
(3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00035
(3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00315
(4-aminophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(4-aminophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00051
(4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00122
(4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.00435
(4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00063
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.00534
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00153
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00226
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00032
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (p-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.23
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (p-tolyl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.00542
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00598
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.00115
(4-chlorophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(4-chlorophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00237
(4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP3
0.00253
(4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
Homo sapiens
pH 9.5, 37°C, NPP1
0.00225
(E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
Homo sapiens
pH 9.5, 37°C, NPP1
0.0124
(R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
(R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
Homo sapiens
pH 9.5, 37°C, NPP1
0.00041
1-(4-aminobenzoyl)-5-methyl-1H-pyrazol-3(2H)-one
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
1-(4-aminobenzoyl)-5-methyl-1H-pyrazol-3(2H)-one
Homo sapiens
pH 9.5, 37°C, NPP1
0.00181
2-[4-[(4-fluorobenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00888
2-[4-[(4-fluorobenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00042
2-[4-[(4-methoxybenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methoxybenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00124
2-[4-[(4-methoxybenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-methoxybenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00029
2-[4-[(4-tert-butylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00071
2-[4-[(4-tert-butylbenzene-1-sulfonyl)oxy]phenyl]-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-yl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00051
3,4,8-tri(4-fluorophenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3,4,8-tri(4-fluorophenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.0207
3,4,8-tri-m-tolyl-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3,4,8-tri-m-tolyl-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00073
3,4,8-tri-p-tolyl-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3,4,8-tri-p-tolyl-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00018
3,4,8-triphenyl-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3,4,8-triphenyl-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00987
3,4,8-tris(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3,4,8-tris(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00126
3,5-dimethyl-4-(naphthalen-2-yloxy)-1H-pyrazole
Homo sapiens
pH 9.5, 37°C, NPP3
0.00804
3,5-dimethyl-4-(naphthalen-2-yloxy)-1H-pyrazole
Homo sapiens
pH 9.5, 37°C, NPP1
0.00063
3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
Homo sapiens
pH 9.5, 37°C, NPP1
0.00242
3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
Homo sapiens
pH 9.5, 37°C, NPP3
0.00039
3,8-dibromo-4-chloro-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP3
0.00765
3,8-dibromo-4-chloro-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.00035
3-(3-bromo-4-chloro-2-(trifluoromethyl)quinolin-8-yl)benzonitrile
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3-(3-bromo-4-chloro-2-(trifluoromethyl)quinolin-8-yl)benzonitrile
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00031
3-bromo-4-chloro-2-(trifluoromethyl)-8-(4-(trifluoromethyl)phenyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3-bromo-4-chloro-2-(trifluoromethyl)-8-(4-(trifluoromethyl)phenyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00025
3-bromo-4-chloro-8-(2,5-dimethoxyphenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.00036
3-bromo-4-chloro-8-(2,5-dimethoxyphenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP3
0.00039
3-bromo-4-chloro-8-(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.00114
3-bromo-4-chloro-8-(4-methoxyphenyl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP3
0.00576
3-bromo-4-chloro-8-(thiophen-3-yl)-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
3-bromo-4-chloro-8-(thiophen-3-yl)-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.00126
3-methyl-2-(4-methylbenzoyl)-1,2-dihydropyrazol-5-one
Homo sapiens
pH 9.5, 37°C, NPP3
0.1
3-methyl-2-(4-methylbenzoyl)-1,2-dihydropyrazol-5-one
Homo sapiens
pH 9.5, 37°C, NPP1
0.00023
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[[4-(trifluoromethyl)benzene-1-sulfonyl]oxy]-1-benzothiophen-2-yl)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.00401
4-(3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-6-[[4-(trifluoromethyl)benzene-1-sulfonyl]oxy]-1-benzothiophen-2-yl)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C
0.000975
4-(4-chlorobenzamido)phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP28
0.001203
4-(4-chlorobenzamido)phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP30
0.003424
4-(4-chlorobenzamido)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP32
0.02157
4-(4-chlorobenzamido)phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP30
0.001437
4-(4-chlorobenzamido)phenyl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP26
0.001624
4-(4-chlorobenzamido)phenyl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP28
0.001525
4-(4-chlorobenzamido)phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP29
0.001799
4-(4-chlorobenzamido)phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP27
0.002772
4-(4-chlorobenzamido)phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP27
0.009614
4-(4-chlorobenzamido)phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP25
0.00281
4-chloro-3,8-diphenyl-2-(trifluoromethyl)quinoline
Homo sapiens
pH 9.5, 37°C, NPP1
0.1
4-chloro-3,8-diphenyl-2-(trifluoromethyl)quinoline
Homo sapiens
above, pH 9.5, 37°C, NPP3
0.000431
4-[(cycloheptanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP19
0.002578
4-[(cycloheptanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP21
0.000255
4-[(cycloheptanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP17
0.000422
4-[(cycloheptanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP15
0.001493
4-[(cycloheptanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP16
0.04701
4-[(cycloheptanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP18
0.006602
4-[(cycloheptanecarbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP16
0.01384
4-[(cycloheptanecarbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP14
0.000387
4-[(cyclohexanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP13
0.00179
4-[(cyclohexanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP15
0.000254
4-[(cyclohexanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP14
0.000564
4-[(cyclohexanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP12
0.000807
4-[(cyclohexanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP13
0.00255
4-[(cyclohexanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP11
0.001079
4-[(cyclohexanecarbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP11
0.01185
4-[(cyclohexanecarbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP9
0.000369
4-[(cyclohexanecarbonyl)amino]phenyl ethanesulfonate
Homo sapiens
pH 9.5, 37°C, NPP9
0.001629
4-[(cyclohexanecarbonyl)amino]phenyl ethanesulfonate
Homo sapiens
pH 9.5, 37°C, NPP7
0.001354
4-[(cyclohexanecarbonyl)amino]phenyl methanesulfonate
Homo sapiens
pH 9.5, 37°C, NPP8
0.001918
4-[(cyclohexanecarbonyl)amino]phenyl methanesulfonate
Homo sapiens
pH 9.5, 37°C, NPP6
0.002409
4-[(cyclohexanecarbonyl)amino]phenyl propane-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP10
0.003461
4-[(cyclohexanecarbonyl)amino]phenyl propane-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP8
0.001134
4-[(cyclopentanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP5
0.003963
4-[(cyclopentanecarbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP7
0.001014
4-[(cyclopentanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP6
0.00576
4-[(cyclopentanecarbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP4
0.000856
4-[(cyclopentanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP4
0.008137
4-[(cyclopentanecarbonyl)amino]phenyl 4-methylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP2
0.001648
4-[(cyclopentanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP3
0.002675
4-[(cyclopentanecarbonyl)amino]phenyl 4-tert-butylbenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP5
0.001724
4-[(cyclopentanecarbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP3
0.04667
4-[(cyclopentanecarbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP1
0.002892
4-[(naphthalene-2-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP36
0.003429
4-[(naphthalene-2-carbonyl)amino]phenyl 2,4,6-tri(propan-2-yl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP34
0.001118
4-[(naphthalene-2-carbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP36
0.005426
4-[(naphthalene-2-carbonyl)amino]phenyl 4-(trifluoromethyl)benzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP38
0.001487
4-[(naphthalene-2-carbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP35
0.01352
4-[(naphthalene-2-carbonyl)amino]phenyl 4-fluorobenzene-1-sulfonate
Homo sapiens
pH 9.5, 37°C, NPP37
0.009296
4-[(naphthalene-2-carbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP31
0.02051
4-[(naphthalene-2-carbonyl)amino]phenyl benzenesulfonate
Homo sapiens
pH 9.5, 37°C, NPP33
0.002
Reactive blue 2
Homo sapiens
-
E-NPP3, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.017
Reactive blue 2
Homo sapiens
-
E-NPP1, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.0012
suramin
Homo sapiens
-
E-NPP3, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
0.0086
suramin
Homo sapiens
-
E-NPP1, in 10 mM HEPES, 1 mM MgCl2, and 2 mM CaCl2, pH 7.4, at 37°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
10
9.5
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4 - 8.5
-
pH 7.4: about 10% of maximal activity, pH 8.5-9.0: maximal activity, NPP1
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
NPP1 is highly expressed in bone, in bone tissue, NPP1 activity is mainly associated with osteoblast- and chondrocyte-derived membrane structures termed matrix vesicles, where it has been identified as the key diphosphate-generating enzyme ensuring normal bone matrix mineralization and soft tissue calcification
-
cDNA clones from patients with Lowe's syndrome, homologue to plasma cell membrane glycoprotein PC-1
additional information
-
strong expression of E-NPP3 in blood serum of colon carcinoma patients
additional information
upregulated expression of NPP1 has been observed in astrocytic brain cancers
additional information
upregulated expression of NPP1 has been observed in astrocytic brain cancers
additional information
-
upregulated expression of NPP1 has been observed in astrocytic brain cancers
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
additional information
-
enriched in matrix vesicles, cytosolic tail motif AAASLLAP is required for correct localization
the mammalian members of the NPP1-3 family are type II (intracellular N-terminus) transmembrane glycoproteins
NPP1 is a homodimeric type II transmembrane glycoprotein with an N-terminal transmembrane domain
additional information
NPP1 is a membrane-associated or secreted enzyme
-
additional information
NPP1 is a membrane-associated or secreted enzyme
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
malfunction
physiological function
additional information
evolution
ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) is a metalloenzyme that belongs to the NPP family, which comprises seven subtypes (NPP1-7)
evolution
ecto-nucleotide pyrophosphatase/phosphodiesterase1 (NPP1) is the most important member of the NPP family, which consists of seven closely related proteins (NPP1-NPP7)
evolution
ecto-nucleotide pyrophosphatase/phosphodiesterase3 (NPP3) belongs to the NPP family, which consists of seven closely related proteins (NPP1-NPP7)
evolution
nucleotide pyrophosphatase/phosphodiesterase (NPP) enzymes belong to the alkaline phosphatase superfamily, with active site characterized by residues of histidine centrally coordinated by divalent cations and serine, cysteine, or threonine residues
malfunction
role for NPP1 in insulin receptor signaling: overexpression of NPP1 increases insulin resistance by desensitization of the insulin receptor. Knockdown of NPP1 with siRNA significantly increases insulin-stimulated phosphorylation of tyrosine kinase in a human hepatoma cell line (HUH7)
malfunction
the blockade of NPP1 can increase the concentration of ATP and 2',3''-cGAMP, but at the same time it can decrease the concentration of adenosine by reducing the concentration of its precursor AMP. This all can lead to an enhancement of the immune response in the body. Lentiviral shRNA-knockdown of NPP1 expression in a human glioblastoma cell line (NCH421k cells) reduces cell proliferation, increased accumulation of cells in the G1/G0 cell cycle phase and induced cell death. The mechanism for this effect may be based on the increased activation of cell apoptosis inducing P2X7 receptor activation owing to the accumulation of undegraded ATP (the main substrate of NPP1) by the knockdown of NPP1 function. Furthermore, the reduced production of extracellular adenosine by a blockade of NPP1 function may also reduce the adenosine induced angiogenesis as well as cell proliferation and differentiation by stimulating P1 receptors. Thus, NPP1 inhibitors may have antineoplastic effects on neuronal tumor cells. Increased expression of NPP1 in the chondrocytes, which is age-related, leads to the overproduction of diphosphate
physiological function
nucleotide pyrophosphatase/phosphodiesterases hydrolyze extracellular nucleotides and dinucleotides and thus control purinergic signaling. EnhancedNPP activity is implicated in health disorders such as osteoarthritis and cancer
physiological function
enzyme NPP1 catalyzes the hydrolysis of a wide range of phosphodiester bonds, e.g. in nucleoside triphosphates, dinucleotides and nucleotide sugars. NPP1 plays a crucial role in various physiological functions including bone mineralization, soft-tissue calcification, and insulin receptor signaling
physiological function
NPP1 is associated with the regulation of extracellular diphosphate levels
physiological function
the enzyme is involved in various biological processes including bone mineralization, soft tissue calcification, insulin receptor signalling, cancer cell proliferation and immune modulation
additional information
homology modelling of human NPP-1 and NPP-3, the structure of mouse Enpp1 (PDB ID 4B56) is used as a template, overview
additional information
homology modelling of human NPP-1 and NPP-3, the structure of mouse Enpp1 (PDB ID 4B56) is used as a template, overview
additional information
-
homology modelling of human NPP-1 and NPP-3, the structure of mouse Enpp1 (PDB ID 4B56) is used as a template, overview
additional information
the active site of NPP1 includes several amino acids such as Ser343, Thr256, Lys295, Phe346, Phe257, Asn277, Tyr340, Lys295, Glu373, Asp376, Tyr451, and His380, they are involved in significant interactions
additional information
the active site of NPP1 includes several amino acids such as Ser343, Thr256, Lys295, Phe346, Phe257, Asn277, Tyr340, Lys295, Glu373, Asp376, Tyr451, and His380, they are involved in significant interactions
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). ITPA_HUMAN
194
0
21446
Swiss-Prot
other Location (Reliability: 2)
ASML_HUMAN
621
0
68857
Swiss-Prot
Mitochondrion (Reliability: 3)
ENPP1_HUMAN
925
1
104924
Swiss-Prot
other Location (Reliability: 1)
ENPP3_HUMAN
875
1
100124
Swiss-Prot
other Location (Reliability: 4)
NUD15_HUMAN
164
0
18609
Swiss-Prot
Mitochondrion (Reliability: 4)
Q9UNI4_HUMAN
26
0
2953
TrEMBL
other Location (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
130000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
homodimer
NPP1 is a homodimeric type II transmembrane glycoprotein characterized by an N-terminal transmembrane domain, two somatomedin-B-like domains, a catalytic domain and a C-terminal nuclease-like domain
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
glycoprotein
-
25% carbohydrate content, only N-glycosidic type oligosaccharides
glycoprotein
-
N-linked oligosaccharides, human 120 kDa-precursor form possesses high-mannose oligosaccharides, which disappear in the mature 130 kDa form
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
K121Q
the mutant is not associated with type 2 diabetes in African Americans
L49A/L50A
-
increase in cellular enzyme activity, redcution of activity in matrix vesicles
L50A
-
increase in cellular enzyme activity, reduction of activity in matrix vesicles
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
gene ENPP1, recombinant expression in COS-7 cells
gene ENPP1, recombinnat expression in COS-7 cells, preparation of memebranes
gene ENPP3, recombinant expression in COS-7 cells, preparation of memebranes
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
enzyme activity in bile is significantly decreased in malignancy, particularly in cholangiocarcinoma
-
upregulated expression of NPP1 has been observed in astrocytic brain cancers
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
NPP1 has been proposed as a drug target for the treatment of glioblastoma
medicine
medicine
variants in the distal region of the ENPP1 gene may contribute to diabetes or diabetic nephropathy susceptibility in African Americans
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Belli, S.I.; Goding, J.W.
Biochemical characterization of human PC-1, an enzyme possessing alkaline phosphodiesterase I and nucleotide pyrophosphatase activities
Eur. J. Biochem.
226
433-443
1994
Homo sapiens, Mus musculus
Yano, T.; Funakoshi, I.; Yamashina, I.
Purification and properties of nucleotide pyrophosphatase from human placenta
J. Biochem.
98
1097-1107
1985
Homo sapiens
Funakoshi, I.; Kato, H.; Horie, K.; Yano, T.; Hori, Y.; Kobayashi, H.; Inoue, T.; Suzuki, H.; Fukui, S.; Tsukahara, M.; Kajii, T.; Yamashina, I.
Molecular cloning of cDNAs for human fibroblast nucleotide pyrophosphatase
Arch. Biochem. Biophys.
295
180-187
1992
Homo sapiens
Yano, T.; Horie, K.; Kanamoto, R.; Kitagawa, H; Funakoshi, I.; Yamashina, I.
Immunoaffinity purification and characterization of nucleotide pyrophosphatase from human placenta
Biochem. Biophys. Res. Commun.
147
1061-1069
1987
Homo sapiens
Vollmayer, P.; Clair, T.; Goding, J.W.; Sano, K.; Servos, J.; Zimmermann, H.
Hydrolysis of diadenosine polyphosphates by nucleotide pyrophosphatases/phosphodiesterases
Eur. J. Biochem.
270
2971-2978
2003
Homo sapiens, Rattus norvegicus (P97675)
Yegutkin, G.G.; Samburski, S.S.; Jalkanen, S.
Soluble purine-converting enzymes circulate in human blood and regulate extracellular ATP level via counteracting pyrophosphatase and phosphotransfer reactions
FASEB J.
17
1328-1330
2003
Homo sapiens
Yano, Y.; Hayashi, Y.; Sano, K.; Shinmaru, H.; Kuroda, Y.; Yokozaki, H.; Yoon, S.; Kasuga, M.
Expression and localization of ecto-nucleotide pyrophosphatase/phosphodiesterase I-3 (E-NPP3/CD203c/PD-I beta/B10/gp130RB13-6) in human colon carcinoma
Int. J. Mol. Med.
12
763-766
2003
Homo sapiens
Vaingankar, S.M.; Fitzpatrick, T.A.; Johnson, K.; Goding, J.W.; Maurice, M.; Terkeltaub, R.
Subcellular targeting and function of osteoblast nucleotide pyrophosphatase phosphodiesterase 1
Am. J. Physiol.
286
C1177-C1187
2004
Homo sapiens, Mus musculus
Yegutkin, G.G.
Nucleotide- and nucleoside-converting ectoenzymes: Important modulators of purinergic signalling cascade
Biochim. Biophys. Acta
1783
673-694
2008
Homo sapiens (O14638), Homo sapiens (P22413)
Keene, K.L.; Mychaleckyj, J.C.; Smith, S.G.; Leak, T.S.; Perlegas, P.S.; Langefeld, C.D.; Freedman, B.I.; Rich, S.S.; Bowden, D.W.; Sale, M.M.
Association of the distal region of the ectonucleotide pyrophosphatase/phosphodiesterase 1 gene with type 2 diabetes in an African-American population enriched for nephropathy
Diabetes
57
1057-1062
2008
Homo sapiens (P22413)
Iqbal, J.; Levesque, S.A.; Sevigny, J.; Mueller, C.E.
A highly sensitive CE-UV method with dynamic coating of silica-fused capillaries for monitoring of nucleotide pyrophosphatase/phosphodiesterase reactions
Electrophoresis
29
3685-3693
2008
Homo sapiens
Eliahu, S.; Lecka, J.; Reiser, G.; Haas, M.; Bigonnesse, F.; Levesque, S.A.; Pelletier, J.; Sevigny, J.; Fischer, B.
Diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors
J. Med. Chem.
53
8485-8497
2010
Homo sapiens, Homo sapiens (O14638), Homo sapiens (P22413)
Poulsen, J.B.; Andersen, K.R.; Kjaer, K.H.; Vestergaard, A.L.; Justesen, J.; Martensen, P.M.
Characterization of human phosphodiesterase 12 and identification of a novel 2-5 oligoadenylate nuclease - The ectonucleotide pyrophosphatase/phosphodiesterase 1
Biochimie
94
1098-1107
2012
Homo sapiens
Duan, R.D.; Hindorf, U.; Cheng, Y.; Bergenzaun, P.; Hall, M.; Hertervig, E.; Nilsson, A.
Changes of activity and isoforms of alkaline sphingomyelinase (nucleotide pyrophosphatase phosphodiesterase 7) in bile from patients undergoing endoscopic retrograde cholangiopancreatography
BMC Gastroenterol.
14
138
2014
Homo sapiens
Lee, S.Y.; Perotti, A.; De Jonghe, S.; Herdewijn, P.; Hanck, T.; Mueller, C.E.
Thiazolo[3,2-a]benzimidazol-3(2H)-one derivatives structure-activity relationships of selective nucleotide pyrophosphatase/phosphodiesterase1 (NPP1) inhibitors
Bioorg. Med. Chem.
24
3157-3165
2016
Homo sapiens (O14638), Homo sapiens (P22413), Homo sapiens
Semreen, M.H.; El-Gamal, M.I.; Ullah, S.; Jalil, S.; Zaib, S.; Anbar, H.S.; Lecka, J.; Sevigny, J.; Iqbal, J.
Synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors
Bioorg. Med. Chem.
27
2741-2752
2019
Homo sapiens (O14638), Homo sapiens (P22413)
Kuhrt, D.; Ejaz, S.A.; Afzal, S.; Khan, S.U.; Lecka, J.; Sevigny, J.; Ehlers, P.; Spannenberg, A.; Iqbal, J.; Langer, P.
Chemoselective synthesis and biological evaluation of arylated 2-(Trifluoromethyl) quinolines as nucleotide pyrophosphatase (NPPs) inhibitors
Eur. J. Med. Chem.
138
816-829
2017
Homo sapiens (O14638), Homo sapiens (P22413)
Channar, P.A.; Afzal, S.; Ejaz, S.A.; Saeed, A.; Larik, F.A.; Mahesar, P.A.; Lecka, J.; Sevigny, J.; Erben, M.F.; Iqbal, J.
Exploration of carboxy pyrazole derivatives synthesis, alkaline phosphatase, nucleotide pyrophosphatase/phosphodiesterase and nucleoside triphosphate diphosphohydrolase inhibition studies with potential anticancer profile
Eur. J. Med. Chem.
156
461-478
2018
Homo sapiens (O14638), Homo sapiens (P22413)
El-Gamal, M.I.; Ullah, S.; Zaraei, S.O.; Jalil, S.; Zaib, S.; Zaher, D.M.; Omar, H.A.; Anbar, H.S.; Pelletier, J.; Sevigny, J.; Iqbal, J.
Synthesis, biological evaluation, and docking studies of new raloxifene sulfonate or sulfamate derivatives as inhibitors of nucleotide pyrophosphatase/phosphodiesterase
Eur. J. Med. Chem.
181
111560
2019
Homo sapiens (O14638), Homo sapiens (P22413)
Lin, S.; McLennan, A.G.; Ying, K.; Wang, Z.; Gu, S.; Jin, H.; Wu, C.; Liu, W.; Yuan, Y.; Tang, R.; Xie, Y.; Mao, Y.
Cloning, expression, and characterization of a human inosine triphosphate pyrophosphatase encoded by the itpa gene
J. Biol. Chem.
276
18695-18701
2001
Homo sapiens (Q9BY32), Homo sapiens
Lee, S.Y.; Mueller, C.E.
Nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) and its inhibitors
MedChemComm
8
823-840
2017
Mus musculus (P06802), Homo sapiens (P22413), Homo sapiens, Rattus norvegicus (Q924C3)
Ausekle, E.; Ejaz, S.A.; Khan, S.U.; Ehlers, P.; Villinger, A.; Lecka, J.; Sevigny, J.; Iqbal, J.; Langer, P.
New one-pot synthesis of N-fused isoquinoline derivatives by palladium-catalyzed C-H arylation potent inhibitors of nucleotide pyrophosphatase-1 and -3
Org. Biomol. Chem.
14
11402-11414
2016
Homo sapiens (O14638), Homo sapiens (P22413), Homo sapiens
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