Reaction Details
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Glycogen synthase kinase-3 alpha
Ligand
BDBM8285
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
2285±103 nM
Citation
Coghlan, MP; Culbert, AA; Cross, DA; Corcoran, SL; Yates, JW; Pearce, NJ; Rausch, OL; Murphy, GJ; Carter, PS; Roxbee Cox, L; Mills, D; Brown, MJ; Haigh, D; Ward, RW; Smith, DG; Murray, KJ; Reith, AD; Holder, 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:
BDBM8285
Synonyms:
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-2,5-dihydro-1H-pyrrole-2,5-dione | 4-arylmaleimide deriv. 7d
Type:
Small organic molecule
Emp. Form.:
C17H13ClN2O2
Mol. Mass.:
312.75
SMILES:
CN(C1=C(C(=O)NC1=O)c1ccc(Cl)cc1)c1ccccc1 |t:2|
Structure:
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3615.87
Organism:
n/a
Description:
n/a
Residue:
32
Sequence:
ITINKYRRAAVPPSPSLSRHSSPHQSPEDEEE