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Literature summary for 3.6.1.9 extracted from

  • 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 (2018), Eur. J. Med. Chem., 156, 461-478 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene ENPP1, recombinant expression in COS-7 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
-
Homo sapiens
(3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
-
Homo sapiens
(3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
-
Homo sapiens
(3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
-
Homo sapiens
(4-aminophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
Homo sapiens
(4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
-
Homo sapiens
(4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
Homo sapiens
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
-
Homo sapiens
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
-
Homo sapiens
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
-
Homo sapiens
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
-
Homo sapiens
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (p-tolyl)methanone
-
Homo sapiens
(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
-
Homo sapiens
(4-chlorophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
-
Homo sapiens
(4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
-
Homo sapiens
(E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
-
Homo sapiens
(R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
-
Homo sapiens
1-(4-aminobenzoyl)-5-methyl-1H-pyrazol-3(2H)-one
-
Homo sapiens
3,5-dimethyl-4-(naphthalen-2-yloxy)-1H-pyrazole
-
Homo sapiens
3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
-
Homo sapiens
3-chloropentane-2,4-dione
-
Homo sapiens
3-methyl-2-(4-methylbenzoyl)-1,2-dihydropyrazol-5-one
-
Homo sapiens
ethyl 3-oxobutanoate
-
Homo sapiens
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 Homo sapiens
Pentane-2,4-dione
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens O14638
-
-
Homo sapiens P22413
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-
K-562 cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl 5'-thymidine monophosphate + H2O
-
Homo sapiens 4-nitrophenol + 5'-thymidine monophosphate
-
?

Synonyms

Synonyms Comment Organism
h-NPP1
-
Homo sapiens
h-NPP3
-
Homo sapiens
NPP1
-
Homo sapiens
NPP3
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
9.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00032
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
0.00035
-
pH 9.5, 37°C, NPP3 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
0.00041
-
pH 9.5, 37°C, NPP3 Homo sapiens 1-(4-aminobenzoyl)-5-methyl-1H-pyrazol-3(2H)-one
0.00051
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
0.00063
-
pH 9.5, 37°C, NPP1 Homo sapiens 3,8-dibromo-2-(trifluoromethyl)quinolin-4(1H)-one
0.00063
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
0.00115
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chlorophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
0.00122
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
0.00126
-
pH 9.5, 37°C, NPP3 Homo sapiens 3,5-dimethyl-4-(naphthalen-2-yloxy)-1H-pyrazole
0.00126
-
pH 9.5, 37°C, NPP3 Homo sapiens 3-methyl-2-(4-methylbenzoyl)-1,2-dihydropyrazol-5-one
0.00153
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
0.00181
-
pH 9.5, 37°C, NPP3 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
0.00225
-
pH 9.5, 37°C, NPP3 Homo sapiens (E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
0.00226
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
0.00237
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
0.00253
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chlorophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
0.00315
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-aminophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
0.00322
-
pH 9.5, 37°C, NPP3 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
0.00342
-
pH 9.5, 37°C, NPP3 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
0.00435
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-aminophenyl) (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)methanone
0.00534
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (4-chlorophenyl)methanone
0.00542
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
0.00598
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
0.00804
-
pH 9.5, 37°C, NPP1 Homo sapiens 3,5-dimethyl-4-(naphthalen-2-yloxy)-1H-pyrazole
0.0124
-
pH 9.5, 37°C, NPP3 Homo sapiens (R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (3,5-dimethyl-1H-pyrazol-1-yl) (pyridin-4-yl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-aminophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-aminophenyl) (3,5-dimethyl-4-(p-tolyloxy)-1H-pyrazol-1-yl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (m-tolyl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (naphthalen-2-yl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (o-tolyl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (p-tolyl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (4-chlorophenyl) (3,5-dimethyl-1H-pyrazol-1-yl)methanone
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (E)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-3-phenylprop-2-en-1-one
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens (R)-1-(4-chloro-3,5-dimethyl-1H-pyrazol-1-yl)-2-(4-isobutylphenyl)propan-1-one
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens 1-(4-aminobenzoyl)-5-methyl-1H-pyrazol-3(2H)-one
0.1
-
pH 9.5, 37°C, NPP1 Homo sapiens 3-methyl-2-(4-methylbenzoyl)-1,2-dihydropyrazol-5-one
0.23
-
pH 9.5, 37°C, NPP3 Homo sapiens (4-chloro-3,5-dimethyl-1H-pyrazol-1-yl) (p-tolyl)methanone

General Information

General Information Comment Organism
physiological function NPP1 is associated with the regulation of extracellular diphosphate levels Homo sapiens