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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