Reaction Details
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Glycogen synthase kinase-3 alpha
Ligand
BDBM8296
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
7.0000±n/a
Temperature
295.1500±n/a K
Ki
9.1±n/a nM
IC50
34.3±n/a 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 | Glycogen synthase kinase 3 alpha (GSKalpha) | Glycogen synthase kinase-3 alpha | Glycogen synthase kinase-3 alpha (GSK3 Alpha) | Glycogen synthase kinase-3 alpha (GSK3A) | Glycogen synthase kinase-3 alpha (GSK3alpha) | GSK3A_HUMAN | GSK3A | Glycogen synthase kinase-3
Type:
Enzyme
Mol. Mass.:
50991.79
Organism:
Human
Description:
P49840
Residue:
483
Sequence:
MSGGGPSGGGPGGSGRARTSSFAEPGGGGGGGGGGPGGSASGPGGTGGGKASVGAMGGGVGASSSGGGPGGSGGGGSGGPGAGTSFPPPGVKLGRDSGKVTTVVATLGQGPERSQEVAYTDIKVIGNGSFGVVYQARLAETRELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDELYLNLVLEYVPETVYRVARHFTKAKLTIPILYVKVYMYQLFRSLAYIHSQGVCHRDIKPQNLLVDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFKSRTPPEAIALCSSLLEYTPSSRLSPLEACAHSFFDELRCLGTQLPNNRPLPPLFNFSAGELSIQPSLNAILIPPHLRSPAGTTTLTPSSQALTETPTSSDWQSTDATPTLTNSS
Inhibitor
Name:
BDBM8296
Synonyms:
CHEMBL102714 | cid_176158 | 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | SB-216763
Type:
Small organic molecule
Emp. Form.:
C19H12Cl2N2O2
Mol. Mass.:
370.03
SMILES:
Cn1cc(C2=C(C(=O)NC2=O)c2ccc(Cl)cc2Cl)c2ccccc12 |t:4|
Substrate
Name:
GSK-3 Peptide Substrate
Synonyms:
GS-1 Peptide | Phospho-GS2 Substrate Peptide
Type:
Peptide
Mol. Mass.:
3045.17
Organism:
n/a
Description:
n/a
Residue:
27
Sequence:
YRRAAVPPSPSLSRHSSPHQSPEDEEE
