Reaction Details Report a problem with these data
Target
Glycogen synthase kinase-3 alpha
Ligand
BDBM8351
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
6±1 nM
Citation
 Witherington, J; Bordas, V; Gaiba, A; Garton, NS; Naylor, A; Rawlings, AD; Slingsby, BP; Smith, DG; Takle, AK; Ward, RW 6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg Med Chem Lett 13:3055-7 (2003) [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:
BDBM8351
Synonyms:
6-aryl-pyrazolo[3,4-b]pyridine analogue 15 | N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Type:
Small organic molecule
Emp. Form.:
C17H16N4O2
Mol. Mass.:
308.3345
SMILES:
Cc1cc2c(NC(=O)C3CC3)n[nH]c2nc1-c1ccc(O)cc1
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