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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

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: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:0030426 (growth cone)
GO:0030529 (intracellular ribonucleoprotein complex)
GO:0030877 (beta-catenin destruction complex)
GO:0043025 (neuronal cell body)
GO:0043197 (dendritic spine)
GO:0043198 (dendritic shaft)
GO:0043227 (membrane-bounded organelle)
GO:0043234 (protein complex)
GO:0044297 (cell body)
GO:0045121 (membrane raft)
GO:0048471 (perinuclear region of cytoplasm)
GO:1990909 (Wnt signalosome)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0001085 (RNA polymerase II transcription factor binding)
GO:0002039 (p53 binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005178 (integrin binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008013 (beta-catenin binding)
GO:0008134 (transcription factor 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:0035255 (ionotropic glutamate receptor binding)
GO:0048156 (tau protein binding)
GO:0050321 (tau-protein kinase activity)
GO:0051059 (NF-kappaB binding)
GO Biological Process GO:0000320 (re-entry into mitotic cell cycle)
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:0006349 (regulation of gene expression by genetic imprinting)
GO:0006468 (protein phosphorylation)
GO:0006611 (protein export from nucleus)
GO:0006983 (ER overload response)
GO:0007163 (establishment or maintenance of cell polarity)
GO:0007212 (dopamine receptor signaling pathway)
GO:0007275 (multicellular organism development)
GO:0007399 (nervous system development)
GO:0007409 (axonogenesis)
GO:0007520 (myoblast fusion)
GO:0007568 (aging)
GO:0007623 (circadian rhythm)
GO:0009887 (organ morphogenesis)
GO:0009968 (negative regulation of signal transduction)
GO:0010226 (response to lithium ion)
GO:0010614 (negative regulation of cardiac muscle hypertrophy)
GO:0010800 (positive regulation of peptidyl-threonine phosphorylation)
GO:0010918 (positive regulation of mitochondrial membrane potential)
GO:0010975 (regulation of neuron projection development)
GO:0010977 (negative regulation of neuron projection development)
GO:0014043 (negative regulation of neuron maturation)
GO:0014823 (response to activity)
GO:0014902 (myotube differentiation)
GO:0016055 (Wnt signaling pathway)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0021766 (hippocampus development)
GO:0030010 (establishment of cell polarity)
GO:0030154 (cell differentiation)
GO:0030516 (regulation of axon extension)
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:0032355 (response to estradiol)
GO:0032436 (positive regulation of proteasomal ubiquitin-dependent protein catabolic process)
GO:0032868 (response to insulin)
GO:0032886 (regulation of microtubule-based process)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0034392 (negative regulation of smooth muscle cell apoptotic process)
GO:0035372 (protein localization to microtubule)
GO:0035556 (intracellular signal transduction)
GO:0035729 (cellular response to hepatocyte growth factor stimulus)
GO:0036016 (cellular response to interleukin-3)
GO:0036018 (cellular response to erythropoietin)
GO:0042493 (response to drug)
GO:0043065 (positive regulation of apoptotic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0043161 (proteasome-mediated ubiquitin-dependent protein catabolic process)
GO:0043407 (negative regulation of MAP kinase activity)
GO:0043525 (positive regulation of neuron apoptotic process)
GO:0043547 (positive regulation of GTPase activity)
GO:0044027 (hypermethylation of CpG island)
GO:0044337 (canonical Wnt signaling pathway involved in positive regulation of apoptotic process)
GO:0045444 (fat cell differentiation)
GO:0045719 (negative regulation of glycogen biosynthetic process)
GO:0045732 (positive regulation of protein catabolic process)
GO:0045773 (positive regulation of axon extension)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046777 (protein autophosphorylation)
GO:0046827 (positive regulation of protein export from nucleus)
GO:0048168 (regulation of neuronal synaptic plasticity)
GO:0048511 (rhythmic process)
GO:0048661 (positive regulation of smooth muscle cell proliferation)
GO:0048814 (regulation of dendrite morphogenesis)
GO:0050770 (regulation of axonogenesis)
GO:0050774 (negative regulation of dendrite morphogenesis)
GO:0051001 (negative regulation of nitric-oxide synthase activity)
GO:0051534 (negative regulation of NFAT protein import into nucleus)
GO:0060070 (canonical Wnt signaling pathway)
GO:0070059 (intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress)
GO:0070301 (cellular response to hydrogen peroxide)
GO:0071109 (superior temporal gyrus development)
GO:0071260 (cellular response to mechanical stimulus)
GO:0071282 (cellular response to iron(II) ion)
GO:0071285 (cellular response to lithium ion)
GO:0071871 (response to epinephrine)
GO:0090090 (negative regulation of canonical Wnt signaling pathway)
GO:0097192 (extrinsic apoptotic signaling pathway in absence of ligand)
GO:0099565 (chemical synaptic transmission, postsynaptic)
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:1901216 (positive regulation of neuron death)
GO:1902065 (response to L-glutamate)
GO:1903351 (cellular response to dopamine)
GO:1904339 (negative regulation of dopaminergic neuron differentiation)
GO:1904885 (beta-catenin destruction complex assembly)
GO:1904886 (beta-catenin destruction complex disassembly)
GO:1990418 (response to insulin-like growth factor stimulus)
GO:1990478 (response to ultrasound)
GO:1990776 (response to angiotensin)
GO:2000077 (negative regulation of type B pancreatic cell development)
GO:2000171 (negative regulation of dendrite development)
GO:2000463 (positive regulation of excitatory postsynaptic potential)
GO:2000466 (negative regulation of glycogen (starch) synthase activity)
GO:2000573 (positive regulation of DNA biosynthetic process)
GO:2000738 (positive regulation of stem cell differentiation)
GO:2001223 (negative regulation of neuron migration)
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.)
UniProt D3DN89 P49841 Q9BWH3 Q9UL47

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
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...