Reaction Details
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Glycogen phosphorylase, liver form
Ligand
BDBM50174389
Substrate
n/a
Meas. Tech.
ChEMBL_321596 (CHEMBL883911)
pH
7.2±n/a
IC50
23±n/a nM
Comments
extracted
Citation
Klabunde, T; Wendt, KU; Kadereit, D; Brachvogel, V; Burger, HJ; Herling, AW; Oikonomakos, NG; Kosmopoulou, MN; Schmoll, D; Sarubbi, E; von Roedern, E; Schönafinger, K; Defossa, E Acyl ureas as human liver glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. J Med Chem 48:6178-93 (2005) [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:
BDBM50174389
Synonyms:
1-(2-Chloro-4-fluoro-benzoyl)-3-(5-hydroxy-2-methoxy-phenyl)-urea | CHEMBL198408 | N-(2-CHLORO-4-FLUOROBENZOYL)-N'-(5-HYDROXY-2-METHOXYPHENYL)UREA
Type:
Small organic molecule
Emp. Form.:
C15H12ClFN2O4
Mol. Mass.:
338.718
SMILES:
COc1ccc(O)cc1NC(=O)NC(=O)c1ccc(F)cc1Cl
Structure:
