Target Validation Information
TTD ID T98062
Target Name Glycogen phosphorylase muscle form (GP)
Type of Target
Patented-recorded
Drug Potency against Target PSN357 Drug Info IC50 = 0.14 nM
1-D-glucopyranosyl cytosine Drug Info Ki = 7700 nM [4]
1-D-glucopyranosyl uracil Drug Info Ki = 6100 nM [4]
2-Hydroxyiminoolean-12-en-28-oic acid Drug Info IC50 = 13100 nM [3]
2-Hydroxyiminours-12-en-28-oic acid Drug Info IC50 = 14700 nM [3]
2-isooleanolic acid Drug Info IC50 = 3500 nM [3]
2-isoursolic acid Drug Info IC50 = 5500 nM [3]
2-Oxoolean-12-en-28-oic acid Drug Info IC50 = 14900 nM [3]
23-hydroxybetulinic acid Drug Info IC50 = 16000 nM [1]
2alpha-Hydroxyolean-12-en-28-oic acid Drug Info IC50 = 8500 nM [3]
2alpha-Hydroxyurs-12-en-28-oic acid Drug Info IC50 = 1200 nM [3]
2beta,3alpha-dihydroxyolean-12-en-28-oic acid Drug Info IC50 = 6250 nM [2]
2beta,3alpha-dihydroxyurs-12-en-28-oic acid Drug Info IC50 = 1100 nM [2]
3alpha-Hydroxyurs-12-en-28-oic Acid Drug Info IC50 = 19000 nM [1]
ASIATIC ACID Drug Info IC50 = 17000 nM [1]
Benzyl 2-hydroxyiminoolean-12-en-28-oate Drug Info IC50 = 16300 nM [3]
BETULIN Drug Info IC50 = 17000 nM [1]
Ethyl 2beta-hydroxyolean-12-en-28-oate Drug Info IC50 = 15300 nM [3]
N-Butyl 2beta-hydroxyolean-12-en-28-oate Drug Info IC50 = 13800 nM [3]
OLEANOLIC_ACID Drug Info IC50 = 14000 nM [1]
Oleanonic acid Drug Info IC50 = 18000 nM [1]
URSOLIC ACID Drug Info IC50 = 15300 nM [3]
Action against Disease Model PSN357 Drug Info Preclinical data also suggest a role for glycogen phosphorylase, as exemplified by the results obtained with GPI-688, PSN-357 and CP-368296 in animal models
References
REF 1 Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystal... J Med Chem. 2008 Jun 26;51(12):3540-54.
REF 2 Practical synthesis of bredemolic acid, a natural inhibitor of glycogen phosphorylase. J Nat Prod. 2008 Nov;71(11):1877-80.
REF 3 Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. J Nat Prod. 2009 Aug;72(8):1414-8.
REF 4 1-(3-Deoxy-3-fluoro-beta-d-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modellin... Bioorg Med Chem. 2010 May 15;18(10):3413-25.

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