Reaction Details Report a problem with these data
Target
Glycogen phosphorylase, liver form
Ligand
BDBM50256712
Substrate
n/a
Meas. Tech.
ChEMBL_515066 (CHEMBL1034808)
IC50
613±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
More Info.:
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:
BDBM50256712
Synonyms:
(2S,3R)-3-(benzyloxy)-2-(3-(3-mesitylureido)-2-naphthamido)-5-methylhexanoic acid | CHEMBL444032
Type:
Small organic molecule
Emp. Form.:
C35H39N3O5
Mol. Mass.:
581.7013
SMILES:
CC(C)C[C@@H](OCc1ccccc1)[C@H](NC(=O)c1cc2ccccc2cc1NC(=O)Nc1c(C)cc(C)cc1C)C(O)=O |r|