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Literature summary extracted from

  • Bennett, S.N.; Campbell, A.D.; Hancock, A.; Johnstone, C.; Kenny, P.W.; Pickup, A.; Plowright, A.T.; Selmi, N.; Simpson, I.; Stocker, A.; Whalley, D.P.; Whittamore, P.R.
    Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 3511-3514.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.4.1.1 drug development the enzyme is a target for inhibitor design in development of drugs for treatment of type 2 diabetes Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.1 (2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 (2-[[(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 (2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 (2-[[(5-chloro-1H-pyrrolo[2,3-c]pyridin-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 (2-[[(5-chloro-6-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 (2-[[(5-chloro-7-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 (2-[[(5-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
 Homo sapiens
2.4.1.1 2-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)-4-methoxybutanoic acid
-
 Homo sapiens
2.4.1.1 3-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)propanoic acid
-
 Homo sapiens
2.4.1.1 3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)amino]-3-oxopropanoic acid
-
 Homo sapiens
2.4.1.1 3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]propanoic acid
-
 Homo sapiens
2.4.1.1 4-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)butanoic acid
-
 Homo sapiens
2.4.1.1 4-[[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfonyl]butanoic acid
-
 Homo sapiens
2.4.1.1 additional information the more active phosphorylated form of the enzyme, glycogen phosphorylase a, is a homodimer having an inhibitory allosteric binding site at the dimer interface for which synthetic ligands Homo sapiens
2.4.1.1 [(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]acetic acid
-
 Homo sapiens
2.4.1.1 [[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfanyl]acetic acid
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.1 [(1->4)-alpha-D-glucosyl]n + phosphate Homo sapiens the liver enzyme catalyzes the forward reaction [(1->4)-alpha-D-glucosyl]n-1 + alpha-D-glucose 1-phosphate
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.1 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.1 [(1->4)-alpha-D-glucosyl]n + phosphate
-
 Homo sapiens [(1->4)-alpha-D-glucosyl]n-1 + alpha-D-glucose 1-phosphate
-
 r
2.4.1.1 [(1->4)-alpha-D-glucosyl]n + phosphate the liver enzyme catalyzes the forward reaction Homo sapiens [(1->4)-alpha-D-glucosyl]n-1 + alpha-D-glucose 1-phosphate
-
 r

Subunits

EC Number Subunits Comment Organism
2.4.1.1 homodimer the more active phosphorylated form, glycogen phosphorylase a, of the enzyme is a homodimer having an inhibitory allosteric binding site at the dimer interface for which synthetic ligands Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.4.1.1 glycogen phosphorylase
-
 Homo sapiens
2.4.1.1 glycogen phosphorylase a
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.1 0.000017
-
 The configuration of the asymmetric centre in the alpha-position of the carboxylic acid is not known. pH and temperature not specified in the publication Homo sapiens 2-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)-4-methoxybutanoic acid
2.4.1.1 0.000018
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.00003
-
 pH and temperature not specified in the publication Homo sapiens [(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]acetic acid
2.4.1.1 0.00004
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.00004
-
 pH and temperature not specified in the publication Homo sapiens [[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfanyl]acetic acid
2.4.1.1 0.000042
-
 pH and temperature not specified in the publication Homo sapiens 4-[[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfonyl]butanoic acid
2.4.1.1 0.000052
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(5-chloro-7-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.000054
-
 pH and temperature not specified in the publication Homo sapiens 4-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)butanoic acid
2.4.1.1 0.000056
-
 pH and temperature not specified in the publication Homo sapiens 3-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)propanoic acid
2.4.1.1 0.000056
-
 pH and temperature not specified in the publication Homo sapiens 3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)amino]-3-oxopropanoic acid
2.4.1.1 0.000057
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.000059
-
 pH and temperature not specified in the publication Homo sapiens 3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]propanoic acid
2.4.1.1 0.000076
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(5-chloro-6-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.00016
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(5-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.00017
-
 The configuration of the asymmetric centre in the alpha-position of the carboxylic acid is not known. pH and temperature not specified in the publication Homo sapiens 2-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)-4-methoxybutanoic acid
2.4.1.1 0.00026
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(5-chloro-1H-pyrrolo[2,3-c]pyridin-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.0012
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
2.4.1.1 0.0015
-
 pH and temperature not specified in the publication Homo sapiens (2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid

General Information

EC Number General Information Comment Organism
2.4.1.1 physiological function glycogen phosphorylase catalyses the breakdown of glycogen to glucose 1-phosphate. In the liver this is metabolized further to glucose which is then secreted into the bloodstream Homo sapiens