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Target
Glycogen phosphorylase, liver form
Ligand
BDBM50256522
Substrate
n/a
Meas. Tech.
ChEMBL_515065 (CHEMBL1034807)
IC50
123±n/a nM
Citation
 Sparks, SM; Banker, P; Bickett, DM; Clancy, DC; Dickerson, SH; Garrido, DM; Golden, PL; Peat, AJ; Sheckler, LR; Tavares, FX; Thomson, SA; Weiel, JE Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues. Bioorg Med Chem Lett 19:981-5 (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:
BDBM50256522
Synonyms:
6,6,6-trifluoro-2-(3-(3-mesitylureido)-2-naphthamido)hexanoic acid | CHEMBL481335
Type:
Small organic molecule
Emp. Form.:
C27H28F3N3O4
Mol. Mass.:
515.5241
SMILES:
Cc1cc(C)c(NC(=O)Nc2cc3ccccc3cc2C(=O)NC(CCCC(F)(F)F)C(O)=O)c(C)c1
Structure:
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