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Target Report Card

Target Name and Classification

Target ID CHEMBL262
Preferred Name Glycogen synthase kinase-3 beta
Synonyms GSK-3 beta | GSK3B | Glycogen synthase kinase-3 beta | Serine/threonine-protein kinase GSK3B
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > cmgc protein kinase group > cmgc protein kinase gsk family

Target Components

Component Description Relationship Accession
Glycogen synthase kinase-3 beta SINGLE PROTEIN P49841

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2095188 Glycogen synthase kinase-3 PROTEIN FAMILY
CHEMBL3883309 Axin-1/Glycogen synthase kinase-3 beta PROTEIN-PROTEIN INTERACTION

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL362558 LY-2090314 Glycogen synthase kinase-3 beta inhibitor 2 PubMed PubMed
CHEMBL3545157 TIDEGLUSIB Glycogen synthase kinase-3 beta inhibitor 2 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000082701
Ensembl ENSG00000082701
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005813 (centrosome)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0030424 (axon)
GO:0030425 (dendrite)
GO:0030877 (beta-catenin destruction complex)
GO:0098794 (postsynapse)
GO:1990909 (Wnt signalosome)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0001085 (RNA polymerase II transcription factor binding)
GO:0002020 (protease binding)
GO:0002039 (p53 binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008013 (beta-catenin binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0031625 (ubiquitin protein ligase binding)
GO:0034236 (protein kinase A catalytic subunit binding)
GO:0034452 (dynactin binding)
GO:0050321 (tau-protein kinase activity)
GO:0051059 (NF-kappaB binding)
GO Biological Process GO:0001837 (epithelial to mesenchymal transition)
GO:0001954 (positive regulation of cell-matrix adhesion)
GO:0005975 (carbohydrate metabolic process)
GO:0005977 (glycogen metabolic process)
GO:0006468 (protein phosphorylation)
GO:0006983 (ER overload response)
GO:0007212 (dopamine receptor signaling pathway)
GO:0007275 (multicellular organism development)
GO:0007399 (nervous system development)
GO:0007623 (circadian rhythm)
GO:0009968 (negative regulation of signal transduction)
GO:0010628 (positive regulation of gene expression)
GO:0010822 (positive regulation of mitochondrion organization)
GO:0016055 (Wnt signaling pathway)
GO:0016310 (phosphorylation)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0021766 (hippocampus development)
GO:0030010 (establishment of cell polarity)
GO:0030011 (maintenance of cell polarity)
GO:0030154 (cell differentiation)
GO:0030516 (regulation of axon extension)
GO:0031175 (neuron projection development)
GO:0031333 (negative regulation of protein complex assembly)
GO:0031334 (positive regulation of protein complex assembly)
GO:0032091 (negative regulation of protein binding)
GO:0032092 (positive regulation of protein binding)
GO:0032436 (positive regulation of proteasomal ubiquitin-dependent protein catabolic process)
GO:0032515 (negative regulation of phosphoprotein phosphatase activity)
GO:0032886 (regulation of microtubule-based process)
GO:0035556 (intracellular signal transduction)
GO:0036016 (cellular response to interleukin-3)
GO:0043066 (negative regulation of apoptotic process)
GO:0043161 (proteasome-mediated ubiquitin-dependent protein catabolic process)
GO:0043547 (positive regulation of GTPase activity)
GO:0045719 (negative regulation of glycogen biosynthetic process)
GO:0045732 (positive regulation of protein catabolic process)
GO:0046777 (protein autophosphorylation)
GO:0046827 (positive regulation of protein export from nucleus)
GO:0048511 (rhythmic process)
GO:0048814 (regulation of dendrite morphogenesis)
GO:0050770 (regulation of axonogenesis)
GO:0060070 (canonical Wnt signaling pathway)
GO:0060079 (excitatory postsynaptic potential)
GO:0070507 (regulation of microtubule cytoskeleton organization)
GO:0070885 (negative regulation of calcineurin-NFAT signaling cascade)
GO:0071109 (superior temporal gyrus development)
GO:0090090 (negative regulation of canonical Wnt signaling pathway)
GO:0097191 (extrinsic apoptotic signaling pathway)
GO:0097192 (extrinsic apoptotic signaling pathway in absence of ligand)
GO:0106028 (neuron projection retraction)
GO:1900034 (regulation of cellular response to heat)
GO:1900181 (negative regulation of protein localization to nucleus)
GO:1901030 (positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathway)
GO:1901215 (negative regulation of neuron death)
GO:1901216 (positive regulation of neuron death)
GO:1901984 (negative regulation of protein acetylation)
GO:1904339 (negative regulation of dopaminergic neuron differentiation)
GO:1904646 (cellular response to beta-amyloid)
GO:1904781 (positive regulation of protein localization to centrosome)
GO:1904885 (beta-catenin destruction complex assembly)
GO:1904886 (beta-catenin destruction complex disassembly)
GO:2000077 (negative regulation of type B pancreatic cell development)
GO:2000466 (negative regulation of glycogen (starch) synthase activity)
Wikipedia GSK3B

Target Cross References - Protein

canSAR P49841
Human Protein Atlas ENSG00000082701
IntAct P49841
Guide to Pharmacology 2030
Open Targets ENSG00000082701
PharmGKB PA29009
Pharos P49841 (Tclin)
Reactome R-HSA-195253 (Degradation of beta-catenin by the destruction complex.)
R-HSA-196299 (Beta-catenin phosphorylation cascade.)
R-HSA-198323 (AKT phosphorylates targets in the cytosol.)
R-HSA-3371453 (Regulation of HSF1-mediated heat shock response.)
R-HSA-399956 (CRMPs in Sema3A signaling.)
R-HSA-4641262 (Disassembly of the destruction complex and recruitment of AXIN to the membrane.)
R-HSA-5250924 (B-WICH complex positively regulates rRNA expression.)
R-HSA-5339716 (Misspliced GSK3beta mutants stabilize beta-catenin.)
R-HSA-5358747 (S33 mutants of beta-catenin aren't phosphorylated.)
R-HSA-5358749 (S37 mutants of beta-catenin aren't phosphorylated.)
R-HSA-5358751 (S45 mutants of beta-catenin aren't phosphorylated.)
R-HSA-5358752 (T41 mutants of beta-catenin aren't phosphorylated.)
R-HSA-5467337 (APC truncation mutants have impaired AXIN binding.)
R-HSA-5467340 (AXIN missense mutants destabilize the destruction complex.)
R-HSA-5467348 (Truncations of AMER1 destabilize the destruction complex.)
R-HSA-5610783 (Degradation of GLI2 by the proteasome.)
R-HSA-5610785 (GLI3 is processed to GLI3R by the proteasome.)
R-HSA-5674400 (Constitutive Signaling by AKT1 E17K in Cancer.)
R-HSA-8939902 (Regulation of RUNX2 expression and activity.)
UniProt D3DN89 P49841 Q9BWH3 Q9UL47

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR033573 (GSK3B.)
Pfam PF00069 (Pkinase)

Target Cross References - Structure

PDBe 1GNG 1H8F 1I09 1J1B 1J1C 1O6K 1O6L 1O9U 1PYX 1Q3D 1Q3W 1Q41 1Q4L 1Q5K 1R0E 1UV5 2JDO 2JDR 2JLD 2O5K 2OW3 2UW9 2X39 2XH5 More...
CREDO 1GNG 1H8F 1I09 1J1B 1J1C 1O6K 1O6L 1O9U 1PYX 1Q3D 1Q3W 1Q41 1Q4L 1Q5K 1R0E 1UV5 2JDO 2JDR 2JLD 2O5K 2OW3 2UW9 2X39 2XH5 More...