Reaction Details Report a problem with these data
Target
Glycogen synthase kinase-3 beta
Ligand
BDBM8147
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
IC50
16±n/a nM
Citation
 Tavares, FX; Boucheron, JA; Dickerson, SH; Griffin, RJ; Preugschat, F; Thomson, SA; Wang, TY; Zhou, HQ N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. J Med Chem 47:4716-30 (2004) [PubMed]  Article 
Target
Name:
Glycogen synthase kinase-3 beta
Synonyms:
GSK-3 beta | GSK-3, beta | GSK3B | GSK3B_HUMAN | Glycogen synthase kinase 3 beta (GSK3B) | Glycogen synthase kinase 3-beta (GSK3B) | Glycogen synthase kinase-3 beta (GSK-3B) | Glycogen synthase kinase-3 beta (GSK3 Beta) | Glycogen synthase kinase-3 beta (GSK3B) | Glycogen synthase kinase-3B (GSK-3B) | Glycogen synthase kinase-3beta (GSK3B) | Serine/threonine-protein kinase GSK3B
Type:
Enzyme
Mol. Mass.:
46756.38
Organism:
Homo sapiens (Human)
Description:
P49841
Residue:
420
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASTPTNATAASDANTGDRGQTNNAASASASNST
  
Inhibitor
Name:
BDBM8147
Synonyms:
3-(2-{[3-(Trifluoromethyl)phenyl]amino}-4-pyrimidin-yl)pyrazolo[1,5-b]pyridazin-6-ol | 5-(2-{[3-(trifluoromethyl)phenyl]amino}pyrimidin-4-yl)pyrazolo[1,5-a]pyridazin-2-ol | pyrazolo[1,5-b]pyridazine deriv. 38
Type:
Small organic molecule
Emp. Form.:
C17H11F3N6O
Mol. Mass.:
372.304
SMILES:
FC(F)(F)c1cccc(Nc2nccc(n2)-c2cnn3[nH]c(=O)ccc23)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
6828.27
Organism:
n/a
Description:
n/a
Residue:
63
Sequence:
ITINAMINHEYLALAALAALALYSARGARGGLILELESERARGARGPRSERPTYRARGAMIDE