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Literature summary for 2.4.1.1 extracted from

  • Onda, K.; Shiraki, R.; Yonetoku, Y.; Momose, K.; Katayama, N.; Orita, M.; Yamaguchi, T.; Ohta, M.; Tsukamoto, S.
    Synthesis and pharmacological evaluation of bis-3-(3,4-dichlorophenyl)acrylamide derivatives as glycogen phosphorylase inhibitors (2008), Bioorg. Med. Chem., 16, 8627-8634.
    View publication on PubMed
Search for more literature for 2.4.1.1

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor (2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide]. Inhibitor is bound at the dimer interface site, the 3,4-dichlorophenyl moiety interacts hydroühobically with the enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E,2'E)-N,N'-(oxydiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
-
 Homo sapiens
(2E,2'E)-N,N'-(thiodiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
-
 Homo sapiens
(2E,2'E)-N,N'-butane-1,4-diylbis[3-(3,4-dichlorophenyl)-acrylamide]
-
 Homo sapiens
(2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide] crystallization data Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P06737
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glycogen + phosphate
-
 Homo sapiens glycogen + alpha-D-glucose 1-phosphate
-
 r

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000012
-
 pH 6.8, 22°C, presence of glucose Homo sapiens (2E,2'E)-N,N'-(thiodiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
0.000023
-
 pH 6.8, 22°C, presence of glucose Homo sapiens (2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide]
0.000026
-
 pH 6.8, 22°C, presence of glucose Homo sapiens (2E,2'E)-N,N'-(oxydiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
0.000043
-
 pH 6.8, 22°C, presence of glucose Homo sapiens (2E,2'E)-N,N'-butane-1,4-diylbis[3-(3,4-dichlorophenyl)-acrylamide]
0.00026
-
 pH 6.8, 22°C Homo sapiens (2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide]
0.00042
-
 pH 6.8, 22°C Homo sapiens (2E,2'E)-N,N'-butane-1,4-diylbis[3-(3,4-dichlorophenyl)-acrylamide]
0.00043
-
 pH 6.8, 22°C Homo sapiens (2E,2'E)-N,N'-(oxydiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
0.00045
-
 pH 6.8, 22°C Homo sapiens (2E,2'E)-N,N'-(thiodiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]