Target
Glycogen phosphorylase, liver form
Ligand
BDBM27726
Substrate
BDBM24362
Meas. Tech.
Human Liver GPa Enzymatic Activity Assay
pH
7.6±n/a
Temperature
298.15±n/a K
IC50
7±n/a 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 Lett 19:1177-82 (2009) [PubMed]  Article 
Target
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:
MAKPLTDQEKRRQISIRGIVGVENVAELKKSFNRHLHFTLVKDRNVATTRDYYFALAHTVRDHLVGRWIRTQQHYYDKCPKRVYYLSLEFYMGRTLQNTMINLGLQNACDEAIYQLGLDIEELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEYGIFNQKIRDGWQVEEADDWLRYGNPWEKSRPEFMLPVHFYGKVEHTNTGTKWIDTQVVLALPYDTPVPGYMNNTVNTMRLWSARAPNDFNLRDFNVGDYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFVVAATLQDIIRRFKASKFGSTRGAGTVFDAFPDQVAIQLNDTHPALAIPELMRIFVDIEKLPWSKAWELTQKTFAYTNHTVLPEALERWPVDLVEKLLPRHLEIIYEINQKHLDRIVALFPKDVDRLRRMSLIEEEGSKRINMAHLCIVGSHAVNGVAKIHSDIVKTKVFKDFSELEPDKFQNKTNGITPRRWLLLCNPGLAELIAEKIGEDYVKDLSQLTKLHSFLGDDVFLRELAKVKQENKLKFSQFLETEYKVKINPSSMFDVQVKRIHEYKRQLLNCLHVITMYNRIKKDPKKLFVPRTVIIGGKAAPGYHMAKMIIKLITSVADVVNNDPMVGSKLKVIFLENYRVSLAEKVIPATDLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENLFIFGMRIDDVAALDKKGYEAKEYYEALPELKLVIDQIDNGFFSPKQPDLFKDIINMLFYHDRFKVFADYEAYVKCQDKVSQLYMNPKAWNTMVLKNIAASGKFSSDRTIKEYAQNIWNVEPSDLKISLSNESNKVNGN
  
Inhibitor
Name:
BDBM27726
Synonyms:
(2S,3R)-3-(tert-butoxy)-2-[(3-{[(2,4,6-trimethylphenyl)carbamoyl]amino}naphthalen-2-yl)formamido]butanoic acid | CHEMBL473851 | anthranilimide based compound, 2
Type:
Small organic molecule
Emp. Form.:
C29H35N3O5
Mol. Mass.:
505.6053
SMILES:
C[C@@H](OC(C)(C)C)[C@H](NC(=O)c1cc2ccccc2cc1NC(=O)Nc1c(C)cc(C)cc1C)C(O)=O |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM24362
Synonyms:
(glucose)n | glycogen
Type:
polymer of glucose
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: