Target
Glycogen synthase kinase-3 alpha
Ligand
BDBM8337
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
pH
7±n/a
Temperature
295.15±n/a K
Ki
0.11±n/a nM
Citation
 Witherington, JBordas, VHaigh, DHickey, DMIfe, RJRawlings, ADSlingsby, BPSmith, DGWard, RW 5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg Med Chem Lett 13:1581-4 (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:
BDBM8337
Synonyms:
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-c]pyridazin-3-yl]cyclopentanecarboxamide | pyrazolopyridazine deriv. 17
Type:
Small organic molecule
Emp. Form.:
C17H15F2N5O
Mol. Mass.:
343.3307
SMILES:
Fc1cccc(c1F)-c1cc2c(NC(=O)C3CCCC3)n[nH]c2nn1
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