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Literature summary for 3.1.3.1 extracted from

  • Li, L.; Chang, L.; Pellet-Rostaing, S.; Liger, F.; Lemaire, M.; Buchet, R.; Wu, Y.
    Synthesis and evaluation of benzo[b]thiophene derivatives as inhibitors of alkaline phosphatases (2009), Bioorg. Med. Chem., 17, 7290-7300.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-2-(benzoylamino)-3-[2-[4-(trifluoromethyl)phenyl]-1-benzothiophen-3-yl]prop-2-enoate with 0.1 mM 35% remaining activity Bos taurus
(4-methoxyphenyl)[2-(4-methoxyphenyl)-1-benzothiophen-3-yl]methanone with 0.1 mM 70% remaining activity Bos taurus
1-(2-phenyl-1-benzothiophen-3-yl)methanamine with 0.4 mM 76% remaining activity Sus scrofa
1-benzothiophen-3-yl 4-fluorophenyl ether with 0.4 mM 78% remaining activity Sus scrofa
1-benzothiophen-3-yl(4-methoxyphenyl)methanone with 0.1 mM 40% remaining activity Bos taurus
1-benzothiophen-3-yl(phenyl)methanone with 0.1 mM 43% remaining activity Bos taurus
2-(1-benzothiophen-2-yl)aniline with 0.4 mM 70% remaining activity Sus scrofa
2-(2-chlorophenyl)-1-benzothiophene-3-carbaldehyde with 0.1 mM 63% remaining activity Bos taurus
2-(2-methylphenyl)-1-benzothiophene-3-carbonitrile with 0.1 mM 5% remaining activity Bos taurus
2-(2-nitrophenyl)-1-benzothiophene-3-carbaldehyde with 0.4 mM 78% remaining activity Sus scrofa
2-(3-chlorophenyl)-1-benzothiophene-3-carbaldehyde with 0.1 mM 62% remaining activity Bos taurus
2-(3-formyl-1-benzothiophen-2-yl)benzonitrile with 0.4 mM 79% remaining activity Sus scrofa
2-(3-methoxy-1-benzothiophen-2-yl)benzonitrile with 0.1 mM 57% remaining activity Bos taurus
2-(3-methoxy-1-benzothiophen-2-yl)benzonitrile with 0.4 mM 79% remaining activity Sus scrofa
2-(3’-pyridine)-3-oxime-benzo[b]thiophene with 0.4 mM 71% remaining activity Sus scrofa
2-(4-chlorophenyl)-1-benzothiophene-3-carbaldehyde with 0.1 mM 9% remaining activity Bos taurus
2-(4-chlorophenyl)-1-benzothiophene-3-carbonitrile with 0.1 mM 69% remaining activity Bos taurus
2-(4-methoxyphenyl)-1-benzothiophene-3-carbaldehyde with 0.1 mM 37% remaining activity Bos taurus
2-(naphthalen-2-yl)-1-benzothiophene-3-carbonitrile with 0.1 mM 18% remaining activity Bos taurus
2-(pyridin-3-yl)-1-benzothiophene-3-carbaldehyde with 0.4 mM 79% remaining activity Sus scrofa
2-iodo-1-benzothiophene with 0.1 mM 41% remaining activity Bos taurus
2-iodo-1-benzothiophene with 0.4 mM 54% remaining activity Sus scrofa
2-phenyl-1-benzothiophene-3-carbaldehyde with 0.1 mM 41% remaining activity Bos taurus
2-phenyl-1-benzothiophene-3-carbaldehyde with 0.4 mM 77% remaining activity Sus scrofa
2-phenyl-1-benzothiophene-3-carbonitrile with 0.1 mM 76% remaining activity Bos taurus
2-phenyl-3-oxime-benzo[b]thiophene with 0.1 mM 1% remaining activity Bos taurus
2-phenyl-3-oxime-benzo[b]thiophene with 0.4 mM 68% remaining activity Sus scrofa
2-phenyl-benzo[b]thiophene-3-carboxylic acid with 0.4 mM 78% remaining activity Sus scrofa
2-[3-(2,2,2-trifluoroethyl)-1-benzothiophen-2-yl]benzonitrile with 0.1 mM 70% remaining activity Bos taurus
2-[3-(4-chlorophenoxy)-1-benzothiophen-2-yl]benzonitrile with 0.4 mM 79% remaining activity Sus scrofa
2-[3-(4-fluorophenoxy)-1-benzothiophen-2-yl]benzonitrile with 0.1 mM 66% remaining activity Bos taurus
2-[4-(1-benzothiophen-3-yl)piperazin-1-yl]phenol with 0.1 mM 49% remaining activity Bos taurus
2-[4-(trifluoromethyl)phenyl]-1-benzothiophene-3-carbaldehyde with 0.1 mM 30% remaining activity Bos taurus
3-(3-methoxy-1-benzothiophen-2-yl)pyridine with 0.4 mM 44% remaining activity Sus scrofa
3-(3-methoxy-1-benzothiophen-2-yl)quinoline with 0.1 mM 64% remaining activity Bos taurus
3-(4-fluorophenoxy)-1-benzothiophene 1-oxide with 0.4 mM 79% remaining activity Sus scrofa
3-methoxy-2-(2-methylphenyl)-1-benzothiophene with 0.1 mM 73% remaining activity Bos taurus
3-methoxy-2-(4-methoxyphenyl)-1-benzothiophene with 0.1 mM 78% remaining activity Bos taurus
4-(1-benzothiophen-3-yloxy)benzaldehyde with 0.1 mM 9% remaining activity Bos taurus
4-[(1-oxido-1-benzothiophen-3-yl)oxy]benzonitrile with 0.4 mM 67% remaining activity Sus scrofa
6-(1-benzothiophen-3-yl)-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole with 0.4 mM 19% remaining activity Sus scrofa
6-(1-benzothiophen-3-yl)-5,6-dihydroimidazo[2,1-b][1,3]thiazole with 0.4 mM 11% remaining activity Sus scrofa
levamisole with 0.4 mM 10% remaining activity Sus scrofa
methyl (2E)-2-(benzoylamino)-3-[2-(4-methoxyphenyl)-1-benzothiophen-3-yl]prop-2-enoate with 0.1 mM 77% remaining activity Bos taurus
methyl 3-(1-benzothiophen-3-yl)-N-benzoylalaninate with 0.4 mM 74% remaining activity Sus scrofa
methyl N-benzoyl-3-[2-[4-(trifluoromethyl)phenyl]-1-benzothiophen-3-yl]alaninate with 0.1 mM 63% remaining activity Bos taurus

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Sus scrofa
-
domestica
-

Purification (Commentary)

Purification (Comment) Organism
commercial product Sus scrofa
commercial product Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
intestine
-
Bos taurus
-
kidney
-
Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
Sus scrofa 4-nitrophenol + phosphate
-
?
4-nitrophenyl phosphate + H2O
-
Bos taurus 4-nitrophenol + phosphate
-
?

Synonyms

Synonyms Comment Organism
alkaline phosphatase
-
Sus scrofa
alkaline phosphatase
-
Bos taurus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.085
-
6-(1-benzothiophen-3-yl)-5,6-dihydroimidazo[2,1-b][1,3]thiazole
-
Sus scrofa
0.093
-
levamisole
-
Sus scrofa
0.135
-
6-(1-benzothiophen-3-yl)-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole
-
Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
aus tab Sus scrofa additional information