dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: S1: Chymotrypsin (type: enzyme)
Target: elastase, neutrophil expressed

Ligand: sivelestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.
Published in: Bioorg Med Chem

Ligand: poststatin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues.
Published in: J Antibiot

Ligand: compound 4g [PMID: 22595175] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.989999771118164 pIC50
Reference (Journal): N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.
Published in: Bioorg Med Chem Lett

Ligand: compound 10l [PMID: 24556381] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.
Published in: Bioorg Med Chem Lett

Ligand: compound 10f [PMID: 24556381] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.369999885559082 pIC50
Reference (Journal): Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.
Published in: Bioorg Med Chem Lett

Ligand: BAY-678 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pKi
Reference (Journal): Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.
Published in: ChemMedChem

Ligand: alvelestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pKi
Reference (Journal): AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase.
Published in: J Pharmacol Exp Ther

Ligand: alpha1-proteinase inhibitor (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity:  -
Target family: S1: Chymotrypsin (type: enzyme)
Target: complement factor B

Ligand: iptacopan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Discovery of 4-((2<i>S</i>,4<i>S</i>)-4-Ethoxy-1-((5-methoxy-7-methyl-1<i>H</i>-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Published in: J Med Chem

Ligand: compound 51 [PMID: 19743866] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Structure-activity relationships for substrate-based inhibitors of human complement factor B.
Published in: J Med Chem
Target family: S1: Chymotrypsin (type: enzyme)
Target: complement C1s

Ligand: sutimlimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2022)
Primary target: yes
Median affinity: 9.59000015258789 pKd
Reference (Patent): Humanized anti-c1s antibodies and methods of use thereof.

Ligand: compound 28 [PMID: 16460935] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pKi
Reference (Journal): A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.
Published in: Bioorg Med Chem Lett
Target family: S1: Chymotrypsin (type: enzyme)
Target: complement C1r

Ligand: nafamostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan only
Primary target: yes
Median affinity: 4.920000076293945 pIC50
Reference (Journal): 2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.
Published in: J Med Chem
Target family: S1: Chymotrypsin (type: enzyme)
Target: coagulation factor XII

Ligand: methyl 5-[(4-tert-butylbenzoyl)amino]-2H-1,2,4-triazole-3-carboxylate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8 pIC50
Reference (Webpage): Factor XIIa 1536 HTS Dose Response Confirmation - BioAssay Summary.

Ligand: garadacimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.819999694824219 pKd
Reference (Patent): Nucleic acids encoding inhibitory anti-factor XII/XIIa monoclonal antibodies

Ligand: anti-FXII nanobody N4-38 (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pKd
Reference (Patent): Anti-fxii nanobody or antigen binding fragment thereof and use thereof
Target family: S1: Chymotrypsin (type: enzyme)
Target: coagulation factor XI

Ligand: osocimab (Antibody)
Interaction type: Antibody
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pKd
Reference (Journal): Allosteric Inhibition as a New Mode of Action for BAY 1213790, a Neutralizing Antibody Targeting the Activated Form of Coagulation Factor XI.
Published in: J Mol Biol

Ligand: milvexian (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.960000038146973 pKi
Reference (Journal): Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Published in: J Med Chem

Ligand: FXIa inhibitor 3f (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.770000457763672 pKi
Reference (Journal): Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Published in: J Med Chem

Ligand: EP-7041 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): EP-7041, a Factor XIa Inhibitor as a Potential Antithrombotic Strategy in Extracorporeal Membrane Oxygenation: A Brief Report.
Published in: Crit Care Explor

Ligand: alpha-ketothiazole analogue 36 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Published in: Bioorg Med Chem

Ligand: abelacimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 11.890000343322754 pKd
Reference (Journal): MAA868 locks factor XIa in a zymogen-like state.
Published in: Blood
Target family: S1: Chymotrypsin (type: enzyme)
Target: coagulation factor VII

Ligand: PCI-27483 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Factor viia inhibitor

Ligand: compound 1 [PMID: 16650987] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Efforts toward oral bioavailability in factor VIIa inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 11 [PMID: 16413183] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Small molecule inhibitors of plasma kallikrein.
Published in: Bioorg Med Chem Lett
Target family: S1: Chymotrypsin (type: enzyme)
Target: coagulation factor IX

Ligand: emicizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 5.800000190734863 pKd
Reference (Journal): Factor VIIIa-mimetic cofactor activity of a bispecific antibody to factors IX/IXa and X/Xa, emicizumab, depends on its ability to bridge the antigens.
Published in: Thromb Haemost

Ligand: compound 57 [PMID: 20121197] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.
Published in: J Med Chem
Target family: S1: Chymotrypsin (type: enzyme)
Target: chymotrypsinogen B1

Ligand: beta ph61 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pKi
Reference (Journal): Enol lactone inhibitors of serine proteases. The effect of regiochemistry on the inactivation behavior of phenyl-substituted (halomethylene)tetra- and -dihydrofuranones and (halomethylene)tetrahydropyranones toward alpha-chymotrypsin: stable acyl enzyme intermediate.
Published in: J Med Chem
Target family: S1: Chymotrypsin (type: enzyme)
Target: chymotrypsin like elastase 2A

Ligand: elafin (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: S1: Chymotrypsin (type: enzyme)
Target: chymotrypsin like elastase 1

Ligand: telaprevir (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Published in: Antimicrob Agents Chemother
Target family: S1: Chymotrypsin (type: enzyme)
Target: chymotrypsin C

Ligand: milvexian (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pKi
Reference (Journal): Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Published in: J Med Chem

Ligand: compound 20 [PMID: 12372533] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.
Published in: Bioorg Med Chem Lett
Target family: S1: Chymotrypsin (type: enzyme)
Target: chymase 1

Ligand: TY-51469 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Chymase inhibition reduces the progression to heart failure after autoimmune myocarditis in rats.
Published in: Exp Biol Med (Maywood)

Ligand: TY-51469 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): The specific chymase inhibitor TY-51469 suppresses the accumulation of neutrophils in the lung and reduces silica-induced pulmonary fibrosis in mice.
Published in: Exp Lung Res

Ligand: NK3201 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): A specific chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[3,4-dioxo-1-phenyl-7-(2-pyridyloxy)]-2-heptyl]acetamide (NK3201), suppresses development of abdominal aortic aneurysm in hamsters.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-10311795 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
Published in: J Med Chem

Ligand: compound 7f [PMID: 29191554] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Structure-based design, synthesis, and binding mode analysis of novel and potent chymase inhibitors.
Published in: Bioorg Med Chem Lett
Target family: S1: Chymotrypsin (type: enzyme)
Target: cathepsin G

Ligand: compound 4g [PMID: 22595175] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.849999904632568 pIC50
Reference (Journal): N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.
Published in: Bioorg Med Chem Lett

Ligand: compound 1 [PMID: 11425539] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
Published in: Bioorg Med Chem Lett

Ligand: aloxistatin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.960000038146973 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
Target family: S1: Chymotrypsin (type: enzyme)
Target: acrosin

Ligand: compound 9 [PMID: 3514912] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.479999542236328 pIC50
Reference (Journal): Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates.
Published in: J Med Chem
Target family: S28: Lysosomal Pro-Xaa carboxypeptidase (type: enzyme)
Target: Dipeptidyl-peptidase 7

Ligand: UAMC00039 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 10.1 pKi
Reference (Journal): Dipeptidyl peptidase II and leukocyte cell death.
Published in: Biochem Pharmacol
Target family: S28: Lysosomal Pro-Xaa carboxypeptidase (type: enzyme)
Target: Prolylcarboxypeptidase

Ligand: compound 35 [PMID: 24157366] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.100000381469727 pIC50
Reference (Journal): Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Published in: Bioorg Med Chem Lett
Target family: S33: Prolyl aminopeptidase (type: enzyme)
Target: protein phosphatase methylesterase 1

Ligand: ABL127 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1.
Published in: J Med Chem

Ligand: ABL127 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.
Published in: Nat Chem Biol
Target family: S33: Prolyl aminopeptidase (type: enzyme)
Target: monoacylglycerol lipase

Ligand: JZL184 (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates.
Published in: Chem Biol

Ligand: ABD-1970 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.
Published in: J Pharmacol Exp Ther
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 9

Ligand: SBC-115,337 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases

Ligand: tafolecimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: China (2023)
Primary target: no
Median affinity:  -
Reference (Patent): Anti-PCSK9 antibody and use thereof
Target family: S8: Subtilisin (type: enzyme)
Target: tripeptidyl peptidase 2

Ligand: peptide 4 [PMID: 18294843] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKi
Reference (Journal): Use of lantibiotic synthetases for the preparation of bioactive constrained peptides.
Published in: Bioorg Med Chem Lett

Ligand: example 8 [WO1999033801A1] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.4399995803833 pKi
Reference (Patent): Tripeptidyl peptidase inhibitors.
Target family: S8: Subtilisin (type: enzyme)
Target: furin, paired basic amino acid cleaving enzyme

Ligand: furin inhibitor peptide (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.639999866485596 pKi
Reference (Journal): Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
Published in: J Biol Chem

Ligand: MI-1148 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 11.260000228881836 pKi
Reference (Journal): Novel Furin Inhibitors with Potent Anti-infectious Activity.
Published in: ChemMedChem

Ligand: peptide 18 [PMID: 24350995] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.369999885559082 pKi
Reference (Journal): Design, synthesis, and structure-activity relationship studies of a potent PACE4 inhibitor.
Published in: J Med Chem

Ligand: phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Published in: J Med Chem
Target family: S8: Subtilisin (type: enzyme)
Target: membrane bound transcription factor peptidase, site 1

Ligand: compound 7b [PMID: 17583500] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Aminopyrrolidineamide inhibitors of site-1 protease.
Published in: Bioorg Med Chem Lett
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 1

Ligand: phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pKi
Reference (Journal): Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Published in: J Med Chem
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 2

Ligand: peptide 18 [PMID: 24350995] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.619999885559082 pKi
Reference (Journal): Design, synthesis, and structure-activity relationship studies of a potent PACE4 inhibitor.
Published in: J Med Chem
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 4

Ligand: furin inhibitor peptide (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.360000133514404 pKi
Reference (Journal): Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
Published in: J Biol Chem
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 5

Ligand: furin inhibitor peptide (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.630000114440918 pKi
Reference (Journal): Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
Published in: J Biol Chem

Ligand: phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Published in: J Med Chem
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 6

Ligand: furin inhibitor peptide (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.789999961853027 pKi
Reference (Journal): Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
Published in: J Biol Chem

Ligand: multi-Leu (ML)-peptide (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.739999771118164 pKi
Reference (Journal): The Multi-Leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells.
Published in: J Med Chem

Ligand: peptide 18 [PMID: 24350995] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pKi
Reference (Journal): Design, synthesis, and structure-activity relationship studies of a potent PACE4 inhibitor.
Published in: J Med Chem

Ligand: phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pKi
Reference (Journal): Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Published in: J Med Chem
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 7

Ligand: furin inhibitor peptide (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pKi
Reference (Journal): Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
Published in: J Biol Chem

Ligand: peptide 18 [PMID: 24350995] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.860000133514404 pKi
Reference (Journal): Design, synthesis, and structure-activity relationship studies of a potent PACE4 inhibitor.
Published in: J Med Chem