Target family: 3.5.1.- Histone deacetylases (HDACs) (type: enzyme)
Target: histone deacetylase 5

Ligand: vorinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2006)
Primary target: no
Median affinity: 5.440000057220459 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: 6.590000152587891 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: 7.010000228881836 pIC50
Reference (Journal): Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.
Published in: Nat Chem Biol

Ligand: SS-208 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.159999847412109 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 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: 6.260000228881836 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: 8.430000305175781 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: pracinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.329999923706055 pIC50
Reference (Journal): SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer.
Published in: Mol Cancer Ther

Ligand: martinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.449999809265137 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: 5.960000038146973 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: 6.21999979019165 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: 6.380000114440918 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: 7.940000057220459 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: CHR-3996 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 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: belinostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 6.760000228881836 pKi
Reference (Journal): Chemical phylogenetics of histone deacetylases.
Published in: Nat Chem Biol