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Target
Glycogen synthase kinase-3 alpha
Ligand
BDBM8278
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
IC50
152±n/a nM
Citation
 Smith, DG; Buffet, M; Fenwick, AE; Haigh, D; Ife, RJ; Saunders, M; Slingsby, BP; Stacey, R; Ward, RW 3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg Med Chem Lett 11:635-9 (2001) [PubMed]  Article 
Target
Name:
Glycogen synthase kinase-3 alpha
Synonyms:
GSK-3 alpha | GSK3A | GSK3A_HUMAN | Glycogen synthase kinase 3 alpha (GSKalpha) | Glycogen synthase kinase-3 | Glycogen synthase kinase-3 alpha | Glycogen synthase kinase-3 alpha (GSK3 Alpha) | Glycogen synthase kinase-3 alpha (GSK3A) | Glycogen synthase kinase-3 alpha (GSK3alpha)
Type:
Enzyme
Mol. Mass.:
50991.79
Organism:
Homo sapiens (Human)
Description:
P49840
Residue:
483
Sequence:
MSGGGPSGGGPGGSGRARTSSFAEPGGGGGGGGGGPGGSASGPGGTGGGKASVGAMGGGVGASSSGGGPGGSGGGGSGGPGAGTSFPPPGVKLGRDSGKVTTVVATLGQGPERSQEVAYTDIKVIGNGSFGVVYQARLAETRELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDELYLNLVLEYVPETVYRVARHFTKAKLTIPILYVKVYMYQLFRSLAYIHSQGVCHRDIKPQNLLVDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFKSRTPPEAIALCSSLLEYTPSSRLSPLEACAHSFFDELRCLGTQLPNNRPLPPLFNFSAGELSIQPSLNAILIPPHLRSPAGTTTLTPSSQALTETPTSSDWQSTDATPTLTNSS
  
Inhibitor
Name:
BDBM8278
Synonyms:
3-{[4-(methylsulfanyl)phenyl]amino}-4-(3-nitrophenyl)-2,5-dihydro-1H-pyrrole-2,5-dione | 4-arylmaleimide deriv. 6ii
Type:
Small organic molecule
Emp. Form.:
C17H13N3O4S
Mol. Mass.:
355.368
SMILES:
CSc1ccc(NC2=C(C(=O)NC2=O)c2cccc(c2)N(=O)=O)cc1 |t:7|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3615.87
Organism:
n/a
Description:
n/a
Residue:
32
Sequence:
ITINKYRRAAVPPSPSLSRHSSPHQSPEDEEE