Target family: 3.5.1.- Histone deacetylases (HDACs) (type: enzyme)
Target: histone deacetylase 4

Ligand: trichostatin A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.849999904632568 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: TMP269 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.
Published in: Nat Chem Biol

Ligand: tasquinimod (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment.
Published in: Cancer Res

Ligand: scriptaid (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.119999885559082 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: no
Median affinity: 6 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: 7.690000057220459 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol

Ligand: quisinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.1899995803833 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: 7.920000076293945 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: martinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.710000038146973 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: KA1010 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.510000228881836 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: 5.980000019073486 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: 7.28000020980835 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: dacinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.650000095367432 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: 7.880000114440918 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: belinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 6.940000057220459 pEC50
Reference (Journal): Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
Published in: Biochem J

Ligand: belinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 6.420000076293945 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol