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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7278
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
200±n/a nM
Comments
extracted
Citation
 Leost, M; Schultz, C; Link, A; Wu, YZ; Biernat, J; Mandelkow, EM; Bibb, JA; Snyder, GL; Greengard, P; Zaharevitz, DW; Gussio, R; Senderowicz, AM; Sausville, EA; Kunick, C; Meijer, L Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem 267:5983-94 (2000) [PubMed]  Article 
Target
Name:
Glycogen synthase kinase-3 beta
Synonyms:
GSK-3, beta | GSK3B_RAT | Glycogen Synthase Kinase-3, beta | Gsk3b
Type:
Enzyme
Mol. Mass.:
46754.43
Organism:
Rattus norvegicus (rat)
Description:
The rat GSK-3 beta cDNA was inserted into the baculovirus vector. The protein was purified from virus-infected sf9 insect cells
Residue:
420
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDMWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASPPANATAASDTNAGDRGQTNNAASASASNST
  
Inhibitor
Name:
BDBM7278
Synonyms:
11-chloropaullone | 16-chloro-8,18-diazatetracyclo[9.7.0.0^{2,7}.0^{12,17}]octadeca-1(11),2,4,6,12(17),13,15-heptaen-9-one | CHEMBL318471 | NSC 672233 | Paullone Analog 17
Type:
Small organic molecule
Emp. Form.:
C16H11ClN2O
Mol. Mass.:
282.724
SMILES:
Clc1cccc2c3CC(=O)Nc4ccccc4-c3[nH]c12
Structure:
Search PDB for entries with ligand similarity:
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