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Target Report Card

Target Name and Classification

Target ID CHEMBL2850
Preferred Name Glycogen synthase kinase-3 alpha
Synonyms GSK-3 alpha | GSK3A | Glycogen synthase kinase-3 alpha | Serine/threonine-protein kinase GSK3A
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 alpha SINGLE PROTEIN P49840

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 alpha inhibitor 2 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000105723
Ensembl ENSG00000105723
GO Cellular Component GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005829 (cytosol)
GO:0005874 (microtubule)
GO:0030877 (beta-catenin destruction complex)
GO:0043025 (neuronal cell body)
GO:0097440 (apical dendrite)
GO:0098794 (postsynapse)
GO:1990635 (proximal dendrite)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005102 (receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0034236 (protein kinase A catalytic subunit binding)
GO:0050321 (tau-protein kinase activity)
GO Biological Process GO:0003073 (regulation of systemic arterial blood pressure)
GO:0003214 (cardiac left ventricle morphogenesis)
GO:0005975 (carbohydrate metabolic process)
GO:0005977 (glycogen metabolic process)
GO:0006349 (regulation of gene expression by genetic imprinting)
GO:0006468 (protein phosphorylation)
GO:0007212 (dopamine receptor signaling pathway)
GO:0007399 (nervous system development)
GO:0007568 (aging)
GO:0008286 (insulin receptor signaling pathway)
GO:0009968 (negative regulation of signal transduction)
GO:0010628 (positive regulation of gene expression)
GO:0010800 (positive regulation of peptidyl-threonine phosphorylation)
GO:0010905 (negative regulation of UDP-glucose catabolic process)
GO:0016055 (Wnt signaling pathway)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0031398 (positive regulation of protein ubiquitination)
GO:0032007 (negative regulation of TOR signaling)
GO:0032436 (positive regulation of proteasomal ubiquitin-dependent protein catabolic process)
GO:0032869 (cellular response to insulin stimulus)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0036016 (cellular response to interleukin-3)
GO:0036498 (IRE1-mediated unfolded protein response)
GO:0043161 (proteasome-mediated ubiquitin-dependent protein catabolic process)
GO:0043525 (positive regulation of neuron apoptotic process)
GO:0044027 (hypermethylation of CpG island)
GO:0045719 (negative regulation of glycogen biosynthetic process)
GO:0045732 (positive regulation of protein catabolic process)
GO:0045823 (positive regulation of heart contraction)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046325 (negative regulation of glucose import)
GO:0046627 (negative regulation of insulin receptor signaling pathway)
GO:0060079 (excitatory postsynaptic potential)
GO:0061052 (negative regulation of cell growth involved in cardiac muscle cell development)
GO:0071285 (cellular response to lithium ion)
GO:0071407 (cellular response to organic cyclic compound)
GO:0071879 (positive regulation of adrenergic receptor signaling pathway)
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:0106071 (positive regulation of adenylate cyclase-activating G-protein coupled receptor signaling pathway)
GO:1901030 (positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathway)
GO:1902004 (positive regulation of beta-amyloid formation)
GO:1903146 (regulation of mitophagy)
GO:1903955 (positive regulation of protein targeting to mitochondrion)
GO:1904227 (negative regulation of glycogen synthase activity, transferring glucose-1-phosphate)
GO:2000077 (negative regulation of type B pancreatic cell development)
GO:2000171 (negative regulation of dendrite development)
GO:2000466 (negative regulation of glycogen (starch) synthase activity)
GO:2000467 (positive regulation of glycogen (starch) synthase activity)
Wikipedia GSK3A

Target Cross References - Protein

canSAR P49840
Human Protein Atlas ENSG00000105723
IntAct P49840
Guide to Pharmacology 2029
Open Targets ENSG00000105723
PharmGKB PA29008
Pharos P49840 (Tclin)
Reactome R-HSA-198323 (AKT phosphorylates targets in the cytosol.)
R-HSA-381038 (XBP1(S) activates chaperone genes.)
R-HSA-5674400 (Constitutive Signaling by AKT1 E17K in Cancer.)
UniProt O14959 P49840

Target Cross References - Domain

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