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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM11442
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
3100±n/a nM
Comments
extracted
Citation
 Voigt, B; Meijer, L; Lozach, O; Schachtele, C; Totzke, F; Hilgeroth, A Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes. Bioorg Med Chem Lett 15:823-5 (2005) [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:
BDBM11442
Synonyms:
5-chloro-N-(4-methanesulfonylphenyl)pyrazolo[1,5-a]pyrimidin-7-amine | sulfonylphenylamino analogue 8a
Type:
Small organic molecule
Emp. Form.:
C13H11ClN4O2S
Mol. Mass.:
322.77
SMILES:
CS(=O)(=O)c1ccc(Nc2cc(Cl)nc3ccnn23)cc1
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