Target family: GSK subfamily (type: enzyme)
Target: glycogen synthase kinase 3 beta

Ligand: AZD1080 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.510000228881836 pKi
Reference (Journal): AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.
Published in: J Neurochem

Ligand: AZD2858 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.3100004196167 pKi
Reference (Journal): Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
Published in: J Med Chem

Ligand: BX-795 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.210000038146973 pIC50
Reference (Journal): Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
Published in: J Biol Chem

Ligand: BX-912 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.130000114440918 pIC50
Reference (Journal): Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
Published in: J Biol Chem

Ligand: Cdk1/5 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: Cdk/Crk inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.119999885559082 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: CHIR-98014 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.239999771118164 pIC50
Reference (Journal): Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
Published in: Diabetes

Ligand: compound 2f [Jiang et al., 2018] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.179999828338623 pIC50
Reference (Journal): Dual GSK-3β/AChE Inhibitors as a New Strategy for Multitargeting Anti-Alzheimer's Disease Drug Discovery.
Published in: ACS Med Chem Lett

Ligand: compound 2 [PMID: 22560567] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.760000228881836 pIC50
Reference (Journal): 6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 4-3 [PMID: 34027661] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.179999828338623 pIC50
Reference (Journal): Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3&#x3b2; Inhibitors for the Treatment of Acute Promyelocytic Leukemia.
Published in: J Med Chem

Ligand: compound 4g [PMID: 2680437] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): Synthesis of Novel Oxazolo[4,5-b]pyridine-2-one based 1,2,3-triazoles as Glycogen Synthase Kinase-3β Inhibitors with Anti-inflammatory Potential.
Published in: Chem Biol Drug Des

Ligand: compound 52 [PMID: 9677190] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: compound 5b [PMID: 24900464] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
Published in: ACS Med Chem Lett

Ligand: compound 5 [PMID: 19338355] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.610000133514404 pIC50
Reference (Journal): From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
Published in: J Med Chem

Ligand: compound 89S [PMID: 19115845] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.840000152587891 pIC50
Reference (Journal): First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.
Published in: J Med Chem

Ligand: elraglusib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
Published in: J Med Chem

Ligand: GNF4877 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Inhibition of DYRK1A and GSK3B induces human β-cell proliferation.
Published in: Nat Commun

Ligand: GSK2646264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pIC50
Reference (Journal): Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.
Published in: Bioorg Med Chem Lett

Ligand: GSK-3β inhibitor 3 [PMID: 25845281] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Journal): Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Published in: Bioorg Med Chem Lett

Ligand: GSK-3beta inhibitor I (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.849999904632568 pIC50
Reference (Journal): Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.
Published in: Bioorg Med Chem Lett

Ligand: GSK-3beta inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.409999847412109 pIC50
Reference (Journal): Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: GSK-3beta inhibitor VIII (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.420000076293945 pKi
Reference (Journal): Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418.
Published in: J Biol Chem

Ligand: GSK-3beta inhibitor XI (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.599999904632568 pKi
Reference (Journal): Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3beta (GSK-3beta) inhibitors.
Published in: Bioorg Med Chem

Ligand: GSK-3 inhibitor IX (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): GSK-3-selective inhibitors derived from Tyrian purple indirubins.
Published in: Chem Biol

Ligand: GSK-3 inhibitor IX (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.
Published in: J Med Chem

Ligand: GSK-3 inhibitor X (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.
Published in: J Med Chem

Ligand: GSK-3 inhibitor XIII (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.659999847412109 pKi
Reference (Journal): The discovery of the potent aurora inhibitor MK-0457 (VX-680).
Published in: Bioorg Med Chem Lett

Ligand: IM-12 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.28000020980835 pIC50
Reference (Journal): Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.
Published in: Bioorg Med Chem

Ligand: indirubin-3'-monoxime (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?
Published in: J Biol Chem

Ligand: isogranulatimide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.
Published in: Mol Cancer Ther

Ligand: isogranulatimide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.300000190734863 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: kenpaullone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?
Published in: J Biol Chem

Ligand: laduviglusib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.170000076293945 pIC50
Reference (Journal): Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
Published in: Diabetes

Ligand: Li+ (Inorganic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1970)
Primary target: no
Median affinity: 2.5999999046325684 pIC50
Reference (Journal): Lithium inhibits glycogen synthase kinase-3 by competition for magnesium.
Published in: Biochem Biophys Res Commun

Ligand: LY2090314 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.960000038146973 pIC50
Reference (Journal): Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Published in: J Med Chem

Ligand: RGB-286638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs.
Published in: Leukemia

Ligand: SB 216763 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Published in: Chem Biol

Ligand: SB-415286 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.420000076293945 pIC50
Reference (Journal): Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Published in: Chem Biol

Ligand: tideglusib (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib.
Published in: J Biol Chem

Ligand: TWS119 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Synthetic small molecules that control stem cell fate.
Published in: Proc Natl Acad Sci USA

Ligand: voruciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pIC50
Reference (Journal): Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells.
Published in: PLoS ONE