Target family: 3.5.1.- Histone deacetylases (HDACs) (type: enzyme)
Target: histone deacetylase 2

Ligand: vorinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2006)
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: trichostatin A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.1899995803833 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: tacedinaline (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: suprastat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.75 pIC50
Reference (Journal): Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.
Published in: J Med Chem

Ligand: scriptaid (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.65999984741211 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: santacruzamate A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.920000076293945 pIC50
Reference (Journal): Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp.
Published in: J Nat Prod

Ligand: romidepsin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009)
Primary target: no
Median affinity: 10.420000076293945 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: ricolinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.
Published in: Blood

Ligand: quisinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.479999542236328 pIC50
Reference (Journal): JNJ-26481585, a novel &quot;second-generation&quot; oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity.
Published in: Clin Cancer Res

Ligand: panobinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2015)
Primary target: no
Median affinity: 8.520000457763672 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: mocetinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.46999979019165 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: martinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs.
Published in: J Med Chem

Ligand: marbostat-100 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.110000133514404 pKi
Reference (Journal): Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
Published in: J Med Chem

Ligand: KA1010 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.809999942779541 pIC50
Reference (Journal): Inhibition of Histone Deacetylase 6 Reveals a Potent Immunosuppressant Effect in Models of Transplantation.
Published in: Transplantation

Ligand: givinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 8.520000457763672 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: givinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 7.25 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: fimepinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling.
Published in: Clin Cancer Res

Ligand: entinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.940000057220459 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: entinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.190000057220459 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: dacinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: CUDC-101 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pIC50
Reference (Journal): Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
Published in: J Med Chem

Ligand: citarinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.349999904632568 pIC50
Reference (Journal): Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.
Published in: Oncotarget

Ligand: CHR-3996 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.
Published in: J Med Chem

Ligand: butyric acid (Metabolite)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.920000076293945 pIC50
Reference (Journal): Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.
Published in: ACS Med Chem Lett

Ligand: BML-281 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.619999885559082 pIC50
Reference (Journal): Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
Published in: J Med Chem

Ligand: belinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 9.069999694824219 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: belinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 6.900000095367432 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: apicidin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: apicidin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.920000076293945 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: ACY-738 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability.
Published in: Neuropsychopharmacology