PMID

Data

Article Title

Organization

Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).

Charles River Discovery Research Services

Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.

Boehringer Ingelheim (Canada)

Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.

Chang Gung University

Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.

Hokkaido University

Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.

Universidade De Lisboa

Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design.

Asubio Pharma

Discovery of potent, selective chymase inhibitors via fragment linking strategies.

Boehringer Ingelheim Pharmaceuticals

Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.

Celera Genomics

Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.

Aarhus University

N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.

University of Lisbon

Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.

Federal University of Alfenas

Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.

Merck Research Laboratories

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.

Cephalon

Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).

Gsk

Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase.

Welfide

Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.

Welfide

Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.

Georgia Institute of Technology

Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.

Boehringer Ingelheim Pharmaceuticals

Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.

Aristotle University of Thessaloniki

Phage-encoded combinatorial chemical libraries based on bicyclic peptides.

Laboratory of Molecular Biology, Medical Research Council

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

Johnson & Johnson Pharmaceutical Research and Development

Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.

Merck Frosst Canada

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

National Human Genome Research Institute

 

Janus compounds: dual inhibitors of proteinases

TBA

Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors.

University of Gda£?Sk

Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.

University of Leipzig

Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.

Daiichi Asubio Pharma

Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.

Daiichi Asubio Pharma

Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.

Johnson & Johnson Pharmaceutical Research and Development

Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.

Shionogi

Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.

Kalvista Pharmaceuticals

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.

Bristol Myers Squibb

Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.

Johnson & Johnson Pharmaceutical Research & Development

Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.

Toa Eiyo

Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Shionogi

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.

Qpex Biopharma

1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.

Shionogi

Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.

Shionogi

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development

Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.

Kyoto Pharmaceutical University

Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.

Nippon Steel

Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.

The University of Queensland

N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.

Nippon Steel

Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.

The University of Queensland

Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.

Proscript

Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.

Glaxowellcome Medicines Research Centre

Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.

Zeneca Pharmaceuticals

Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.

RhôNe-Poulenc Rorer

Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective.

Indian Institute of Technology (Bhu)

Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.

Suntory

Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.

The University of Queensland

Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.

Zeneca Pharmaceuticals

Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.

Thrombosis Research Institute

New orally active serine protease inhibitors.

Minase Research Institute

Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.

Zeneca Pharmaceuticals

On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients.

Virginia Commonwealth University

Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G.

Merrell Dow Research Institute

Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold.

The University of Queensland

Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.

Bicycle Therapeutics

Benzoxazinone derivatives for treatment of skin diseases

Sixera Pharma