Reaction Details Report a problem with these data
Target
Glycogen phosphorylase, liver form
Ligand
BDBM24385
Substrate
BDBM24362
Meas. Tech.
Enzyme Inhibition Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
7±n/a nM
Citation
Birch, AM; Kenny, PW; Oikonomakos, NG; Otterbein, L; Schofield, P; Whittamore, PR; Whalley, DP Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors. Bioorg Med Chem Lett 17:394-9 (2007) [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:
Human
Description:
Dimers associate into a tetramer to form the enzymatically active phosphorylase A.
Residue:
847
Sequence:
MAKPLTDQEKRRQISIRGIVGVENVAELKKSFNRHLHFTLVKDRNVATTRDYYFALAHTVRDHLVGRWIRTQQHYYDKCPKRVYYLSLEFYMGRTLQNTMINLGLQNACDEAIYQLGLDIEELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEYGIFNQKIRDGWQVEEADDWLRYGNPWEKSRPEFMLPVHFYGKVEHTNTGTKWIDTQVVLALPYDTPVPGYMNNTVNTMRLWSARAPNDFNLRDFNVGDYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFVVAATLQDIIRRFKASKFGSTRGAGTVFDAFPDQVAIQLNDTHPALAIPELMRIFVDIEKLPWSKAWELTQKTFAYTNHTVLPEALERWPVDLVEKLLPRHLEIIYEINQKHLDRIVALFPKDVDRLRRMSLIEEEGSKRINMAHLCIVGSHAVNGVAKIHSDIVKTKVFKDFSELEPDKFQNKTNGITPRRWLLLCNPGLAELIAEKIGEDYVKDLSQLTKLHSFLGDDVFLRELAKVKQENKLKFSQFLETEYKVKINPSSMFDVQVKRIHEYKRQLLNCLHVITMYNRIKKDPKKLFVPRTVIIGGKAAPGYHMAKMIIKLITSVADVVNNDPMVGSKLKVIFLENYRVSLAEKVIPATDLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENLFIFGMRIDDVAALDKKGYEAKEYYEALPELKLVIDQIDNGFFSPKQPDLFKDIINMLFYHDRFKVFADYEAYVKCQDKVSQLYMNPKAWNTMVLKNIAASGKFSSDRTIKEYAQNIWNVEPSDLKISLSNESNKVNGN
Inhibitor
Name:
BDBM24385
Synonyms:
2,3-dichloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-4H-thieno[3,2-b]pyrrole-5-carboxamide | 3,4-dihydro-2-quinolone (DHQ) derivative, 24
Type:
Small organic molecule
Emp. Form.:
C18H15Cl2N3O3S
Mol. Mass.:
424.301
SMILES:
OCCN1C(=O)C(Cc2ccccc12)NC(=O)c1cc2sc(Cl)c(Cl)c2[nH]1