Target family: 3.5.1.- Histone deacetylases (HDACs) (type: enzyme)
Target: histone deacetylase 8

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

Ligand: vorinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2006)
Primary target: no
Median affinity:  pKi
Reference (Journal): Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
Published in: Bioorg Med Chem Lett

Ligand: tubastatin A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.090000152587891 pIC50
Reference (Patent): HDAC inhibitors and therapeutic methods of using same

Ligand: trichostatin A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: SZUH280 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas.
Published in: Leukemia

Ligand: suprastat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 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: SS-208 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.909999847412109 pIC50
Reference (Journal): Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
Published in: J Med Chem

Ligand: scriptaid (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.980000019073486 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: romidepsin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009)
Primary target: no
Median affinity: 9.819999694824219 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 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: resminostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.059999942779541 pIC50
Reference (Journal): The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells.
Published in: Br J Haematol

Ligand: quisinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.369999885559082 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: 6.610000133514404 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: marbostat-100 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.760000228881836 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: 6.440000057220459 pIC50
Reference (Journal): Inhibition of Histone Deacetylase 6 Reveals a Potent Immunosuppressant Effect in Models of Transplantation.
Published in: Transplantation

Ligand: J27644 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pIC50
Reference (Journal): Discovery of HDAC6, HDAC8, and 6/8 Inhibitors and Development of Cell-Based Drug Screening Models for the Treatment of TGF-&#x3b2;-Induced Idiopathic Pulmonary Fibrosis.
Published in: J Med Chem

Ligand: givinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 7.409999847412109 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: droxinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.840000152587891 pIC50
Reference (Journal): Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands.
Published in: Mol Cancer Ther

Ligand: dacinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.46999979019165 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: 7.099999904632568 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: compound 25ap [PMID: 37796543] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pIC50
Reference (Journal): Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
Published in: J Med Chem

Ligand: citarinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.860000133514404 pIC50
Reference (Journal): Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.
Published in: Oncotarget

Ligand: butyric acid (Metabolite)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.820000171661377 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: 5.090000152587891 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: 7.599999904632568 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: 6.670000076293945 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: 7.309999942779541 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: apicidin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.239999771118164 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J