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TargetGlycogen phosphorylase, liver form
LigandBDBM27745
Substrate/CompetitorBDBM24362
Meas. Tech.Human Liver GPa Enzymatic Activity Assay
pH7.6±n/a
Temperature298.15±n/a K
IC50 4±1 nM
Citation Thomson, SABanker, PBickett, DMBoucheron, JACarter, HLClancy, DCCooper, JPDickerson, SHGarrido, DMNolte, RTPeat, AJSheckler, LRSparks, SMTavares, FXWang, LWang, TYWeiel, JE Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy. Bioorg Med Chem Lett19:1177-82 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Glycogen phosphorylase, liver form
Name:Glycogen phosphorylase, liver form
Synonyms:Glycogen Phosphorylase (PYGL) | Glycogen Phosphorylase, liver form | Liver glycogen phosphorylase | PYGL | PYGL_HUMAN
Type:Homodimer
Mol. Mass.:97153.98
Organism:Homo sapiens (Human)
Description:Dimers associate into a tetramer to form the enzymatically active phosphorylase A.
Residue:847
Sequence:
MAKPLTDQEKRRQISIRGIVGVENVAELKKSFNRHLHFTLVKDRNVATTRDYYFALAHTV
RDHLVGRWIRTQQHYYDKCPKRVYYLSLEFYMGRTLQNTMINLGLQNACDEAIYQLGLDI
EELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEYGIFNQKIRDGWQVEEA
DDWLRYGNPWEKSRPEFMLPVHFYGKVEHTNTGTKWIDTQVVLALPYDTPVPGYMNNTVN
TMRLWSARAPNDFNLRDFNVGDYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFV
VAATLQDIIRRFKASKFGSTRGAGTVFDAFPDQVAIQLNDTHPALAIPELMRIFVDIEKL
PWSKAWELTQKTFAYTNHTVLPEALERWPVDLVEKLLPRHLEIIYEINQKHLDRIVALFP
KDVDRLRRMSLIEEEGSKRINMAHLCIVGSHAVNGVAKIHSDIVKTKVFKDFSELEPDKF
QNKTNGITPRRWLLLCNPGLAELIAEKIGEDYVKDLSQLTKLHSFLGDDVFLRELAKVKQ
ENKLKFSQFLETEYKVKINPSSMFDVQVKRIHEYKRQLLNCLHVITMYNRIKKDPKKLFV
PRTVIIGGKAAPGYHMAKMIIKLITSVADVVNNDPMVGSKLKVIFLENYRVSLAEKVIPA
TDLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENLFIFGMRIDDVA
ALDKKGYEAKEYYEALPELKLVIDQIDNGFFSPKQPDLFKDIINMLFYHDRFKVFADYEA
YVKCQDKVSQLYMNPKAWNTMVLKNIAASGKFSSDRTIKEYAQNIWNVEPSDLKISLSNE
SNKVNGN
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BDBM27745
BDBM24362
NameBDBM27745
Synonyms:(2S,3R)-3-(tert-butoxy)-2-[(2-{[(2,6-dimethyl-4-propylphenyl)carbamoyl]amino}-4-(4-methoxyphenyl)phenyl)formamido]butanoic acid | anthranilimide based compound, 21
TypeSmall organic molecule
Emp. Form.C34H43N3O6
Mol. Mass.589.7217
SMILESCCCc1cc(C)c(NC(=O)Nc2cc(ccc2C(=O)N[C@@H]([C@@H](C)OC(C)(C)C)C(O)=O)-c2ccc(OC)cc2)c(C)c1 |r|
Structure
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