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TargetGlycogen phosphorylase, liver form
LigandBDBM27729
Substrate/CompetitorBDBM24362
Meas. Tech.Human Liver GPa Enzymatic Activity Assay
pH7.6±n/a
Temperature298.15±n/a K
IC50 10±7 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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BDBM27729
BDBM24362
NameBDBM27729
Synonyms:(2S,3R)-3-(tert-butoxy)-2-[(4-phenyl-2-{[(2,4,6-trimethylphenyl)carbamoyl]amino}phenyl)formamido]butanoic acid | anthranilimide based compound, 5
TypeSmall organic molecule
Emp. Form.C31H37N3O5
Mol. Mass.531.6426
SMILESC[C@@H](OC(C)(C)C)[C@H](NC(=O)c1ccc(cc1NC(=O)Nc1c(C)cc(C)cc1C)-c1ccccc1)C(O)=O |r|
Structure
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