Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7275
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
130±n/a nM
Comments
extracted
Citation
 Leost, MSchultz, CLink, AWu, YZBiernat, JMandelkow, EMBibb, JASnyder, GLGreengard, PZaharevitz, DWGussio, RSenderowicz, AMSausville, EAKunick, CMeijer, 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:
BDBM7275
Synonyms:
14-methyl-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 | 9-methylpaullone | CHEMBL317964 | NSC 675995 | Paullone Analog 14
Type:
Small organic molecule
Emp. Form.:
C17H14N2O
Mol. Mass.:
262.3059
SMILES:
Cc1ccc2[nH]c-3c(CC(=O)Nc4ccccc-34)c2c1
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