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TargetGlycogen phosphorylase, liver form
LigandBDBM27731
Substrate/CompetitorBDBM24362
Meas. Tech.Human Liver GPa Enzymatic Activity Assay
pH7.6±n/a
Temperature298.15±n/a K
IC50 8±3 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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BDBM27731
BDBM24362
NameBDBM27731
Synonyms:(2S,3R)-3-(tert-butoxy)-2-{[4-(3-methoxyphenyl)-2-{[(2,4,6-trimethylphenyl)carbamoyl]amino}phenyl]formamido}butanoic acid | anthranilimide based compound, 7
TypeSmall organic molecule
Emp. Form.C32H39N3O6
Mol. Mass.561.6686
SMILESCOc1cccc(c1)-c1ccc(C(=O)N[C@@H]([C@@H](C)OC(C)(C)C)C(O)=O)c(NC(=O)Nc2c(C)cc(C)cc2C)c1 |r|
Structure
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