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Literature summary for 2.7.7.48 extracted from

  • Wang, G.; Lim, S.P.; Chen, Y.L.; Hunziker, J.; Rao, R.; Gu, F.; Seh, C.C.; Ghafar, N.A.; Xu, H.; Chan, K.; Lin, X.; Saunders, O.L.; Fenaux, M.; Zhong, W.; Shi, P.Y.; Yokokawa, F.
    Structure-activity relationship of uridine-based nucleoside phosphoramidate prodrugs for inhibition of dengue virus RNA-dependent RNA polymerase (2018), Bioorg. Med. Chem. Lett., 28, 2324-2327 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2'-C-ethynyl-2'-fluoro-uridine triphosphate
-
Dengue virus type 2
2'-C-ethynyl-4'-fluoro-uridine triphosphate
-
Dengue virus type 2
2'-C-ethynyl-uridine triphosphate
-
Dengue virus type 2
2'-C-methyl-4'-fluoro-uridine triphosphate
-
Dengue virus type 2
2'-C-methyl-uridine triphosphate
-
Dengue virus type 2
2'-C-propynyl-4'-fluoro-uridine triphosphate
-
Dengue virus type 2
2'-C-propynyl-uridine triphosphate
-
Dengue virus type 2
propan-2-yl (2S)-2-([([(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxy-4-(prop-1-yn-1-yl)oxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
-
Dengue virus type 2
propan-2-yl (2S)-2-([([(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxy-4-methyloxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
-
Dengue virus type 2
propan-2-yl (2S)-2-([([(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-ethynyl-3,4-dihydroxyoxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
-
Dengue virus type 2
propan-2-yl (2S)-2-([([(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-fluoro-3,4-dihydroxy-4-(prop-1-yn-1-yl)oxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
-
Dengue virus type 2
propan-2-yl (2S)-2-([([(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-fluoro-3,4-dihydroxy-4-methyloxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
-
Dengue virus type 2
propan-2-yl (2S)-2-([([(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-ethynyl-2-fluoro-3,4-dihydroxyoxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate the prodrug displays potent anti-dengue virus activity in the primary human peripheral blood mononuclear cell-based assay with no significant cytotoxicity in human hepatocellular liver carcinoma cell lines and no mitochondrial toxicity in the cell-based assay using human prostate cancer cell lines Dengue virus type 2
sofosbuvir
-
Dengue virus type 2
sofosbuvir triphosphate
-
Dengue virus type 2

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
nucleoside triphosphate + RNAn Dengue virus type 2
-
diphosphate + RNAn+1
-
?

Organism

Organism UniProt Comment Textmining
Dengue virus type 2
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
nucleoside triphosphate + RNAn
-
Dengue virus type 2 diphosphate + RNAn+1
-
?

Synonyms

Synonyms Comment Organism
RNA-dependent RNA polymerase
-
Dengue virus type 2

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00019
-
pH and temperature not specified in the publication Dengue virus type 2 propan-2-yl (2S)-2-([([(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxy-4-methyloxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
0.00045
-
pH and temperature not specified in the publication Dengue virus type 2 propan-2-yl (2S)-2-([([(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-ethynyl-3,4-dihydroxyoxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
0.00057
-
pH and temperature not specified in the publication Dengue virus type 2 propan-2-yl (2S)-2-([([(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-ethynyl-2-fluoro-3,4-dihydroxyoxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
0.00065
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-ethynyl-4'-fluoro-uridine triphosphate
0.0011
-
pH and temperature not specified in the publication Dengue virus type 2 propan-2-yl (2S)-2-([([(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-fluoro-3,4-dihydroxy-4-methyloxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
0.0012
-
pH and temperature not specified in the publication Dengue virus type 2 sofosbuvir
0.0016
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-ethynyl-uridine triphosphate
0.0019
-
pH and temperature not specified in the publication Dengue virus type 2 propan-2-yl (2S)-2-([([(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxy-4-(prop-1-yn-1-yl)oxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
0.002
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-propynyl-uridine triphosphate
0.0028
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-propynyl-4'-fluoro-uridine triphosphate
0.005
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-methyl-uridine triphosphate
0.0066
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-methyl-4'-fluoro-uridine triphosphate
0.009
-
pH and temperature not specified in the publication Dengue virus type 2 propan-2-yl (2S)-2-([([(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-fluoro-3,4-dihydroxy-4-(prop-1-yn-1-yl)oxolan-2-yl]methoxy)(phenoxy)phosphoryl]amino)propanoate
0.0159
-
pH and temperature not specified in the publication Dengue virus type 2 2'-C-ethynyl-2'-fluoro-uridine triphosphate
0.018
-
pH and temperature not specified in the publication Dengue virus type 2 sofosbuvir triphosphate