PMID

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Article Title

Organization

Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.

Baylor University

Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.

The University of Tokyo

Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.

Universitat Jaume I

Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.

Cnrs

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

Charles River Discovery Research Services

Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.

Whitman College

Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.

University of Bonn

Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.

Baylor University

Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.

Hebei University of Science & Technology

SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.

Kurukshetra University

Structure-based design and optimization of potent inhibitors of the adenoviral protease.

Novartis Institute For Biomedical Research

8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.

Array Biopharma

Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.

Universidade Federal De S£O Carlos

The discovery of potent, selective, and reversible inhibitors of the house dust mite peptidase allergen Der p 1: an innovative approach to the treatment of allergic asthma.

Domainex

3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.

University of Bonn

Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors.

E£Tv£S Lor£Nd University (Elte)

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.

Astrazeneca

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

Hokkaido University

Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.

Kurukshetra University

Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.

University of Ljubljana

Discovery of novel cyanamide-based inhibitors of cathepsin C.

TBA

Design of selective Cathepsin inhibitors.

Astrazeneca

Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.

Celera Genomics

Fluorescent nitrile-based inhibitors of cysteine cathepsins.

University of Bonn

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research and Development

Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases.

TBA

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.

Astrazeneca

(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.

Astrazeneca

Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.

University of Bonn

Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.

Hokkaido University

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.

Astrazeneca

Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.

TBA

Exploring activity cliffs in medicinal chemistry.

Rheinische Friedrich-Wilhelms-Universit£T

Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.

University of Bonn

Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.

Universit£

Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.

Universit£

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University of Florida

Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.

Federal University of Alfenas

Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.

Ewha Womans University

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 trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.

University of California

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Johnson & Johnson Pharmaceutical Research & Development

Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain.

Pukyong National University

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.

University of Messina

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

Merck Frosst Centre For Therapeutic Research

Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.

Santhera Pharmaceuticals

Protease inhibitors: current status and future prospects.

University of Queensland

Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.

Takeda Chemical Industries

D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.

Cephalon

Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.

Maxim Pharmaceuticals

Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.

Boehringer Ingelheim Pharmaceuticals

 

Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L

TBA

Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors.

National Chemical Laboratory (Csir-Ncl)

Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.

University of Messina

Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B.

University of Ljubljana

Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.

Boehringer Ingelheim (Canada)

1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.

Merck Research Laboratories

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.

Merck Research Laboratories

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.

Merck Research Laboratories

Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.

Baylor University

Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.

Merck Research Laboratories

Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.

Georgia Institute of Technology

MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.

Merck Research Laboratories

Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.

University of WüRzburg

2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.

Merck Research Laboratories

On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.

University of Duisburg-Essen

Dioxo-triazines as a novel series of cathepsin K inhibitors.

Schering-Plough

Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.

Schering-Plough

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

Merck Frosst Canada

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.

Baylor University

Structure-guided development of selective TbcatB inhibitors.

University of California

 

Nonpeptidic inhibitors of recombinant human calpain I

TBA

 

Oligopresentation of protease inhibitors with β-cyclodextrin as template

TBA

 

Inhibition of human erythrocyte calpain I by novel quinolinecarboxamides

TBA

 

Design of a new selective cysteine protease inactivator and its mechanistic implications

TBA

Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.

University of Messina

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.

Astrazeneca

Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.

University of Toyama

Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.

Bar-Ilan University

Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.

The University of Tennessee Health Science Center

Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.

Korea Research Institute of Chemical Technology

Substrate optimization for monitoring cathepsin C activity in live cells.

Genomics Institute of The Novartis Research Foundation

Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.

LinköPing University

Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.

University of Pennsylvania

Primary amides as selective inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.

The Genomics Institute of The Novartis Research Foundation

Design of potent inhibitors of human beta-secretase. Part 2.

Pfizer

Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.

The University of Tennessee Health Science Center

Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.

China Pharmaceutical University

Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.

Celera Genomics

Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.

Anhui Medical University

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.

Celera

Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.

Arpida

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

Shionogi

Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.

The University of Sydney

Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2.

China Pharmaceutical University

Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.

Shandong University

The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.

Niddk

A novel series of urea-based peptidomimetic calpain inhibitors.

The University of Tennessee Health Science Center

Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.

Celera Genomics

Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

Glaxosmithkline

Azepanone-based inhibitors of human cathepsin L.

Glaxosmithkline

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.

University of Alberta Edmonton

Acyclic cyanamide-based inhibitors of cathepsin K.

Glaxosmithkline

A structural screening approach to ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

New peptidomimetic rhodesain inhibitors with improved selectivity towards human cathepsins.

Johannes Gutenberg University

Novel and potent cyclic cyanamide-based cathepsin K inhibitors.

Glaxosmithkline

Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.

Kyushu University

Covalent sortase A inhibitor ML346 prevents

Shanghai Institute of Materia Medica

Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.

Shandong University

Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.

Université

A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.

Boehringer Ingelheim (Canada)

Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).

University of Southern California

P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.

Eli Lilly

Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.

Glaxosmithkline

Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.

Merck Frosst Centre For Therapeutic Research

Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.

Glaxosmithkline

Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies.

Johannes Gutenberg University

Discovery and

Anhui Medical University

P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.

Eli Lilly

(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.

Amgen

N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.

Novartis Institute of Biomedical Research

Nitrile-based peptoids as cysteine protease inhibitors.

University of S£O Paulo

3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.

Ligand Pharmaceuticals

Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.

Abbott

Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.

University of Tennessee Health Science Center

Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.

Senju Pharmaceutical

N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.

University of Bonn

Synthesis and matched molecular pair analysis of covalent reversible inhibitors of the cysteine protease CPB.

S£O Carlos Institute of Chemistry-University of S£O Paulo (Iqsc-Usp)

Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.

National Research Council of Canada

6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.

Currently Naeja Pharmaceutical

Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.

Currently Naeja Pharmaceutical

Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against ?-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble A? peptide formation.

Ewha Womans University

General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.

University of California

Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.

Celera

Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.

University of Gda£?Sk

Optimization of the

Novartis Pharma

Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.

Pfizer

Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.

Abbott

Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.

University of California

Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.

University of S£O Paulo

Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.

Novartis Pharmaceuticals

Cytotoxicity of 4-substituted quinoline derivatives: Anticancer and antileishmanial potential.

Universidade De Mogi Das Cruzes (Umc)

Potent reversible inhibitors of the protein tyrosine phosphatase CD45.

Astrazeneca Pharmaceuticals

Azepanone-based inhibitors of human and rat cathepsin K.

Glaxosmithkline

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

Merck Frosst Centre For Therapeutic Research

Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.

The University of Tennessee Health Science Center

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

Roche Pharma Research and Early Development

Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.

Knoll

Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.

Brown University

Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.

National Institute of Biological Sciences (Nibs)

Naturally Occurring Lumazines.

University of Auckland

Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.

Jilin University

Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.

Boehringer Ingelheim (Canada)

P2-proline-derived inhibitors of calpain I.

Cephalon

Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.

Boehringer Ingelheim (Canada)

Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe.

Ku Leuven

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

Proscript

Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.

Texas A&M University

Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor.

University of Nebraska Medical Center

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.

Smithkline Beecham Pharmaceuticals

Cathepsin B: Active site mapping with peptidic substrates and inhibitors.

University of Bonn

Peptidomimetic inhibitors of the human cytomegalovirus protease.

Boehringer Ingelheim

Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?

University of S£O Paulo

Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments.

University of Houston

Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.

Georgia Institute of Technology

Development of a potent and selective cell penetrant Legumain inhibitor.

Queen'S University Belfast

The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.

University of California

Development of cell-active non-peptidyl inhibitors of cysteine cathepsins.

The City University of New York

Chalcones, inhibitors for topoisomerase I and cathepsin B and L, as potential anti-cancer agents.

Cha University

Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?

National Institute of Biology

Small-molecule inhibitors of cathepsin L incorporating functionalized ring-fused molecular frameworks.

Baylor University

Vinyl sulfones as mechanism-based cysteine protease inhibitors.

Khepri Pharmaceuticals

Two new carbazole alkaloids from Murraya koenigii.

Chinese Academy of Sciences

New aziridine-based inhibitors of cathepsin L-like cysteine proteases with selectivity for the Leishmania cysteine protease LmCPB2.8.

Johannes Gutenberg-Universit£T Mainz

Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.

Universit£

Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates.

Universitat Jaume I

Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.

Irbm Science Park

Cathepsin B inhibitors: Further exploration of the nitroxoline core.

University of Ljubljana

Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.

Eth Zurich

Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer's Disease: 2-(3-Phenyl-1H-pyrazol-1-yl)-nicotinamides.

Abbvie Deutschland

Idiopathic Pulmonary Fibrosis: Current Status, Recent Progress, and Emerging Targets.

Taipei Medical University

In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.

Balikesir University

 

Design, synthesis and evaluation of trisubstituted thiazoles targeting plasmodium falciparum cysteine proteases

University, Mississippi

Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.

Abbott Laboratories

Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.

Abbott Laboratories

RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Roche Bioscience