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Literature summary for 2.4.1.1 extracted from

  • Onda, K.; Shiraki, R.; Ogiyama, T.; Yokoyama, K.; Momose, K.; Katayama, N.; Orita, M.; Yamaguchi, T.; Furutani, M.; Hamada, N.; Takeuchi, M.; Okada, M.; Ohta, M.; Tsukamoto, S.
    Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors (2008), Bioorg. Med. Chem., 16, 10001-10012.
    View publication on PubMed
Search for more literature for 2.4.1.1

Inhibitors

Inhibitors Comment Organism Structure
5-chloro-N-(1,3,6,6-tetrafluoro-(R)-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide docking study. Hydrophobic residues, such as Phe53, Pro188, and Gly186, around the two aliphatic fluorine atoms suggest that the lipophilic contact among them is an important driver of activity increases. Hydrophobic residues Leu39 and Lys191 are close to one of the aromatic fluorine atoms Homo sapiens
5-chloro-N-(1,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-(1-hydroxy-2,3-dihydro-1H-inden-5-yl)-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-(3,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
 Homo sapiens
5-chloro-N-(6,6-difluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 phosphorylase a
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte primary culture Mus musculus
-
hepatocyte primary culture Homo sapiens
-
liver
-
 Mus musculus
-
liver
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
-
 Homo sapiens 5-chloro-N-(1,3,6,6-tetrafluoro-(R)-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
0.000048
-
-
 Homo sapiens 5-chloro-N-(1,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
0.000063
-
-
 Homo sapiens 5-chloro-N-(3,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
0.000068
-
-
 Homo sapiens 5-chloro-N-(6,6-difluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
0.00032
-
-
 Homo sapiens 5-chloro-N-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
0.00044
-
-
 Homo sapiens 5-chloro-N-(1-hydroxy-2,3-dihydro-1H-inden-5-yl)-1H-indole-2-carboxamide