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Target
Glycogen phosphorylase, liver form
Ligand
BDBM50136437
Substrate
n/a
Meas. Tech.
ChEMBL_424360 (CHEMBL909563)
IC50
86±n/a nM
Citation
Whittamore, PR; Addie, MS; Bennett, SN; Birch, AM; Butters, M; Godfrey, L; Kenny, PW; Morley, AD; Murray, PM; Oikonomakos, NG; Otterbein, LR; Pannifer, AD; Parker, JS; Readman, K; Siedlecki, PS; Schofield, P; Stocker, A; Taylor, MJ; Townsend, LA; Whalley, DP; Whitehouse, J Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies. Bioorg Med Chem Lett 16:5567-71 (2006) [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:
BDBM50136437
Synonyms:
5-Chloro-1H-indole-2-carboxylic acid (2-oxo-1,2,3,4-tetrahydro-quinolin-3-yl)-amide | 5-chloro-N-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-1H-indole-2-carboxamide | CHEMBL139461
Type:
Small organic molecule
Emp. Form.:
C18H14ClN3O2
Mol. Mass.:
339.776
SMILES:
Clc1ccc2[nH]c(cc2c1)C(=O)NC1Cc2ccccc2NC1=O