Target family: T1: Proteasome (type: enzyme)
Target: proteasome 20S subunit beta 5

Ligand: zetomipzomib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.159999847412109 pIC50
Reference (Journal): Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide).
Published in: J Med Chem

Ligand: WLL-vs (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Structure- and function-based design of Plasmodium-selective proteasome inhibitors.
Published in: Nature

Ligand: oprozomib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
Published in: J Med Chem

Ligand: oprozomib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Molecular mechanisms of acquired proteasome inhibitor resistance.
Published in: J Med Chem

Ligand: NIC-0102 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 pIC50
Reference (Journal): Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.
Published in: J Med Chem

Ligand: MG-132 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 pKi
Reference (Journal): Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
Published in: J Med Chem

Ligand: ixazomib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: yes
Median affinity: 9.029999732971191 pKi
Reference (Journal): Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.
Published in: Cancer Res

Ligand: compound 3b [PMID: 24946214] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pKi
Reference (Journal): Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.
Published in: Eur J Med Chem

Ligand: carfilzomib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2015)
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
Published in: J Med Chem

Ligand: bortezomib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2003), EMA (2004)
Primary target: yes
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors.
Published in: Bioorg Med Chem Lett