Literature summary for 2.4.1.1 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.

Search for more literature for 2.4.1.1

Application

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

Inhibitors

Inhibitors	Comment	Organism	Structure
(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-[[(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid	-	Homo sapiens
(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid	-	Homo sapiens
(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-[[(5-chloro-6-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid	-	Homo sapiens
(2-[[(5-chloro-7-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid	-	Homo sapiens
(2-[[(5-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid	-	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	-	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	-	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	-	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	-	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	-	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	-	Homo sapiens
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-[[(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-[[(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)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
[(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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
liver	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
[(1->4)-alpha-D-glucosyl]n + phosphate	-	Homo sapiens	[(1->4)-alpha-D-glucosyl]n-1 + alpha-D-glucose 1-phosphate	-	r
[(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

Subunits	Comment	Organism
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

Synonyms	Comment	Organism
glycogen phosphorylase	-	Homo sapiens
glycogen phosphorylase a	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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

General Information	Comment	Organism
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

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Release 2023.1 (January 2023)