Target
Glycogen synthase kinase-3 alpha
Ligand
BDBM8289
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
460±26 nM
Citation
 Coghlan, MPCulbert, AACross, DACorcoran, SLYates, JWPearce, NJRausch, OLMurphy, GJCarter, PSRoxbee Cox, LMills, DBrown, MJHaigh, DWard, RWSmith, DGMurray, KJReith, ADHolder, JC Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol 7:793-803 (2000) [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:
BDBM8289
Synonyms:
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | 4-arylmaleimide deriv. 8d
Type:
Small organic molecule
Emp. Form.:
C18H13ClN2O2
Mol. Mass.:
324.761
SMILES:
Clc1cccc(c1)C1=C(N2CCc3ccccc23)C(=O)NC1=O |c:8|
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