Target family: C1: Papain (type: enzyme)
Target: cathepsin L

Ligand: CAA0225 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Characterization of CAA0225, a novel inhibitor specific for cathepsin L, as a probe for autophagic proteolysis.
Published in: Biol Pharm Bull

Ligand: compound 4d [PMID: 38746883] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): Identification of Dual Inhibitors Targeting Main Protease (M<sup>pro</sup>) and Cathepsin L as Potential Anti-SARS-CoV-2 Agents.
Published in: ACS Med Chem Lett

Ligand: GC-376 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.359999656677246 pIC50
Reference (Journal): Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.
Published in: ACS Pharmacol Transl Sci

Ligand: K777 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells.
Published in: ACS Chem Biol

Ligand: KGP94 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.900000095367432 pIC50
Reference (Journal): Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
Published in: Bioorg Med Chem Lett

Ligand: LHVS (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Published in: J Biol Chem

Ligand: MG-101 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.1899995803833 pKi
Reference (Journal): Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors.
Published in: J Med Chem

Ligand: Mpro inhibitor 13b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.53000020980835 pKi
Reference (Journal): Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors.
Published in: J Med Chem

Ligand: UAWJ9-36-3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pIC50
Reference (Journal): Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.
Published in: ACS Pharmacol Transl Sci

Ligand: VBY-825 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model.
Published in: Biochimie