Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: enhancer of zeste 2 polycomb repressive complex 2 subunit

Ligand: EPZ005687 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.619999885559082 pKi
Reference (Journal): A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
Published in: Nat Chem Biol

Ligand: EPZ011989 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pKi
Reference (Journal): EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.
Published in: ACS Med Chem Lett

Ligand: GSK126 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
Published in: Nature

Ligand: GSK126 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.
Published in: J Biomol Screen

Ligand: GSK343 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Published in: ACS Med Chem Lett

Ligand: JQEZ5 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pIC50
Reference (Journal): An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation.
Published in: Nat Med

Ligand: PF-06821497 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 pKi
Reference (Journal): Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
Published in: J Med Chem

Ligand: SKLB-03220 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.760000228881836 pIC50
Reference (Journal): Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.
Published in: J Med Chem

Ligand: tazemetostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
Published in: Proc Natl Acad Sci USA

Ligand: tulmimetostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.699999809265137 pIC50
Reference (Patent): Ezh2 inhibition in combination therapies for the treatment of cancers

Ligand: tulmimetostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.960000038146973 pKi
Reference (Patent): Ezh2 inhibition in combination therapies for the treatment of cancers

Ligand: UNC1999 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
Published in: ACS Chem Biol

Ligand: valemetostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2022)
Primary target: no
Median affinity: 8.289999961853027 pIC50
Reference (Journal): Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.
Published in: Cancer Sci