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Literature summary for 3.1.3.11 extracted from

  • Tsukada, T.; Tamaki, K.; Tanaka, J.; Takagi, T.; Yoshida, T.; Okuno, A.; Shiiki, T.; Takahashi, M.; Nishi, T.
    A prodrug approach towards the development of tricyclic-based FBPase inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 2938-2941.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-[[(2R,4S)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
4-[[(2R,4S)-4-(3-methoxyphenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
4-[[(2R,4S)-4-(4-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
4-[[(2S,4S)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
4-[[(2S,4S)-4-(3-methoxyphenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
4-[[(2S,4S)-4-(4-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
6,7-dimethyl-4-[[(2R,4S)-2-oxido-4-(pyridin-2-yl)-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
6,7-dimethyl-4-[[(2R,4S)-2-oxido-4-(pyridin-3-yl)-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
6,7-dimethyl-4-[[(2R,4S)-2-oxido-4-(pyridin-4-yl)-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
6,7-dimethyl-4-[[(2R,4S)-4-(2-methylpyridin-3-yl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
6,7-dimethyl-4-[[(2R,4S)-4-(6-methylpyridin-3-yl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
-
Hominoidea
ethyl (2S,6S)-4-[[(6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazol-4-yl)oxy]methyl]-2,6-dimethyl-7-oxo-8-oxa-3,5-diaza-4-phosphadecan-1-oate 4-oxide
-
Hominoidea

Organism

Organism UniProt Comment Textmining
Hominoidea
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte
-
Hominoidea
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-fructose 1,6-bisphosphate + H2O
-
Hominoidea D-fructose 6-phosphate + phosphate
-
?

Synonyms

Synonyms Comment Organism
FBPase
-
Hominoidea
fructose 1,6-bisphosphatase muscle isoenzyme Hominoidea

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.004
-
shows weak CYP3A4 inhibitor potency Hominoidea 6,7-dimethyl-4-[[(2R,4S)-4-(2-methylpyridin-3-yl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
0.0068
-
-
Hominoidea ethyl (2S,6S)-4-[[(6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazol-4-yl)oxy]methyl]-2,6-dimethyl-7-oxo-8-oxa-3,5-diaza-4-phosphadecan-1-oate 4-oxide
0.0088
-
-
Hominoidea 6,7-dimethyl-4-[[(2R,4S)-2-oxido-4-(pyridin-3-yl)-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
0.011
-
-
Hominoidea 6,7-dimethyl-4-[[(2R,4S)-4-(2-methylpyridin-3-yl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
0.015
-
-
Hominoidea 4-[[(2R,4S)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
0.022
-
-
Hominoidea 6,7-dimethyl-4-[[(2R,4S)-2-oxido-4-(pyridin-2-yl)-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
0.041
-
-
Hominoidea 6,7-dimethyl-4-[[(2R,4S)-2-oxido-4-(pyridin-4-yl)-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole
0.066
-
-
Hominoidea 4-[[(2R,4S)-4-(4-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
0.1
-
value above Hominoidea 4-[[(2S,4S)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
0.1
-
value above Hominoidea 4-[[(2S,4S)-4-(4-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
0.1
-
value above Hominoidea 4-[[(2R,4S)-4-(3-methoxyphenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
0.1
-
value above Hominoidea 4-[[(2S,4S)-4-(3-methoxyphenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-6,7-dimethyl-8H-indeno[1,2-d][1,3]thiazole
0.1
-
value above Hominoidea 6,7-dimethyl-4-[[(2R,4S)-4-(6-methylpyridin-3-yl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy]-8H-indeno[1,2-d][1,3]thiazole