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  2. ANTIVIRAL HETEROARYL KETONE DERIVATIVESBDB
    WIPO WO2022013684 (2022)
    PFIZER INC.
    06/09/22
  3. NOVEL CORONAVIRUS MAIN PROTEASE INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOFBDB
    WIPO WO2022021841 (2022)
    SICHUAN UNIVERSITY
    06/09/22
  4. Potent Inhibition of SARS-CoV-2 nsp14 BDB
    J Med Chem 65: 6231-6249 (2022)
    University of Montpellier
    05/17/22
  5. Aminocarbamoyl compounds for the treatment of viral infectionsBDB
    WIPO WO2022043374 (2022)
    F. Hoffmann-La Roche Ag
    03/30/22
  6. A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.BDB
    Nature (2022)
    University of British Columbia
    03/30/22
  7. Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).EBI
    J Med Chem 63: 13205-13227 (2020)
    South China Agricultural University
    03/27/22
  8.  
    Discovery of S-217622, a Non-Covalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19BDB
    bioRxiv 2022: (2022)
    Shionogi Pharmaceutical Research Center
    02/02/22
  9. Sars-cov-2 inhibitors having covalent modifications for treating coronavirus infectionsBDB
    WIPO WO2021219089 (2021)
    Insilico Medicine Ip Limited
    01/27/22
  10. Perspectives on SARS-CoV-2 Main Protease Inhibitors.BDB
    J Med Chem 64: 16922-16955 (2021)
    Michigan State University
    01/27/22
  11. Inhibitors of cysteine proteases and methods of use thereofBDB
    US Patent US11124497 (2021)
    Pardes Biosciences, Inc.
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  12. Compounds and method of treating covid-19BDB
    WIPO WO2021205290 (2021)
    Pfizer Inc.
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  13. Compounds and methods for the treatment of covid-19BDB
    WIPO WO2021205298 (2021)
    Pfizer Inc.
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  14. Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity.BDB
    J Am Chem Soc 143: 20697-20709 (2021)
    The University of Arizona
    01/13/22
  15. Nitrile-containing antiviral compoundsBDB
    WIPO WO2021250648 (2021)
    Pfizer Inc.
    01/13/22
  16. Design of SARS-CoV-2 PLpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity.BDB
    J Med Chem (2021)
    University of Illinois at Chicago
    11/05/21
  17. Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure-Activity Relationship, and X-ray Structural Studies.BDB
    J Med Chem 64: 14702-14714 (2021)
    Purdue University
    11/05/21
  18. A patent review on SARS coronavirus main protease (3CLpro) inhibitors.BDB
    ChemMedChem (2021)
    Experimental Drug Development Centre
    11/05/21
  19.  
    An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19BDB
    Science 374: 1-13 (2021)
    Pfizer
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  20.  
    Open Science Discovery of Oral Non-Covalent SARS-CoV-2 Main Protease Inhibitor TherapeuticsBDB
    bioRxiv 2021: (2021)
    Israel Institution of Biological Research
    11/05/21
  21. DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 MBDB
    Proc Natl Acad Sci U S A 118: (2021)
    Baylor College of Medicine
    09/11/21
  22. Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.BDB
    ACS Med Chem Lett 12: 1325-1332 (2021)
    Yale University
    09/10/21
  23. 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.BDB
    ACS Pharmacol Transl Sci 4: 1408-1421 (2021)
    The University of Arizona
    09/10/21
  24. Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CLBDB
    J Med Chem 64: (2021)
    Cleveland Clinic
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  25. Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.EBI
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    Qpex Biopharma, Inc.
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  26. Structure-Guided Design of Conformationally Constrained Cyclohexane Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3CL Protease.BDB
    J Med Chem 64: 10047-10058 (2021)
    Wichita State University
    07/29/21
  27. A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.BDB
    Bioorg Med Chem Lett 48: 128263 (2021)
    A*STAR
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  28. Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral PotencyBDB
    ACS Med Chem Lett 12: 1325-1332 (2021)
    Yale University
    07/29/21
  29. Peptidomimetic ?-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and BDB
    J Med Chem (2021)
    University of Alberta
    07/29/21
  30. Highly active compounds against COVID-19BDB
    US Patent US10874687 (2020)
    Atea Pharmaceuticals, Inc.
    07/25/21
  31. N4-hydroxycytidine and derivatives and anti-viral uses related theretoBDB
    US Patent US10874683 (2020)
    Emory University
    07/25/21
  32. SARS-CoV-2 Mpro inhibitors with antiviral activity in a transgenic mouse modelBDB
    Science (2021)
    Sichuan University
    02/28/21
  33.  
    Potent Noncovalent Inhibitors of the Main Protease of SARS-CoV-2 from Molecular Sculpting of the Drug Perampanel Guided by Free Energy Perturbation CalculationsBDB
    ACS Cent Sci (2021)
    Yale University
    02/28/21
  34. Identification and design of novel small molecule inhibitors against MERS-CoV papain-like protease via high-throughput screening and molecular modeling.EBI
    Bioorg Med Chem 27: 1981-1989 (2019)
    University of Illinois at Chicago
    02/24/21
  35. The Other Angiotensin II Receptor: ATEBI
    J Med Chem 63: 1978-1995 (2020)
    Centre Hospitalier Universitaire Vaudois (CHUV) and University of Lausanne (UNIL)
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  36.  
    Identification of inhibitors of SARS-CoV-2 3CL-Pro enzymatic activity using a small molecule in-vitro repurposing screenBDB
    bioRxiv 2020: (2020)
    Fraunhofer Institute for Translational Medicine and Pharmacology (ITMP) and Fraunhofer Cluster of Excellence for Immune mediated diseases (CIMD)
    01/31/21
  37.  
    Inhibition of SARS-CoV-2 main protease by allosteric drug-bindingBDB
    bioRxiv 2020: (2020)
    Center for Free-Electron Laser Science
    01/31/21
  38. A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease InhibitorsBDB
    ChemMedChem (2020)
    Texas A&M University
    01/31/21
  39. Anticoronaviral compounds and compositions, their pharmaceutical uses and materials for their synthesisBDB
    WIPO WO2006061714 (2006)
    Pfizer Inc.
    01/31/21
  40. An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice.BDB
    Sci Transl Med 12: 1-15 (2020)
    University of North Carolina at Chapel Hill
    11/13/20
  41. Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.BDB
    Antimicrob Agents Chemother 64: (2020)
    Institut Pasteur Korea
    11/13/20
  42. The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.BDB
    Med Res Rev (2020)
    University of Bonn
    11/07/20
  43. An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.BDB
    J Med Chem 59: 6595-628 (2016)
    University of Bonn
    11/07/20
  44. Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesisBDB
    WIPO WO2005113580 (2005)
    Pfizer Inc.
    10/17/20
  45. Broad-spectrum non-covalent coronavirus protease inhibitorsBDB
    US Patent US9975885 (2018)
    PURDUE RESEARCH FOUNDATION
    09/25/20
  46. Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.BDB
    bioRxiv (2020)
    National Institutes of Health
    09/21/20
  47.  
    Discovery of potent inhibitors of PLproCoV2 by screening a library of selenium-containing compoundsBDB
    bioRxiv 1-12 (2020)
    University ofAmsterdam
    09/21/20
  48. Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved ?-ketoamide inhibitors.BDB
    Science 368: 409-412 (2020)
    University of Lubeck
    09/21/20
  49. Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease.BDB
    Science 368: 1331-1335 (2020)
    Shanghai Institute of Materia Medica
    09/21/20
  50. Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19.BDB
    bioRxiv (2020)
    Pfizer Inc.
    09/21/20
  51. Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease.BDB
    ACS Infect Dis 6: 2099-2109 (2020)
    University of Georgia
    09/21/20
  52. Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.BDB
    Biochem Biophys Res Commun 333: 194-9 (2005)
    National Taiwan University
    09/21/20
  53. The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis.BDB
    Cancer Discov 4: 1310-25 (2014)
    Fred Hutchinson Cancer Research Center
    09/21/20
  54. Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors BDB
    Nature 582: 289-293 (2020)
    ShanghaiTech University
    09/06/20
  55. 3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice.BDB
    Sci Transl Med 12: (2020)
    Wichita State University
    09/06/20
  56. Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.EBI
    Bioorg Med Chem 22: 292-302 (2014)
    Tianjin University of Science and Technology
    09/02/20
  57. Identification of novel drug scaffolds for inhibition of SARS-CoV 3-Chymotrypsin-like protease using virtual and high-throughput screenings.EBI
    Bioorg Med Chem 22: 167-77 (2014)
    University of Illinois at Chicago
    09/02/20
  58. Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.EBI
    Bioorg Med Chem 21: 3730-7 (2013)
    Korea Research Institute of Bioscience and Biotechnology
    09/01/20
  59. Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors.EBI
    Bioorg Med Chem Lett 23: 6317-20 (2013)
    Kansas State University
    09/01/20
  60. Design, synthesis and crystallographic analysis of nitrile-based broad-spectrum peptidomimetic inhibitors for coronavirus 3C-like proteases.EBI
    Eur J Med Chem 59: 1-6 (2013)
    The Chinese University of Hong Kong
    08/31/20
  61. Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors.EBI
    Bioorg Med Chem 18: 7849-54 (2010)
    Academia Sinica
    08/28/20
  62. Biflavonoids from Torreya nucifera displaying SARS-CoV 3CL(pro) inhibition.EBI
    Bioorg Med Chem 18: 7940-7 (2010)
    Korea Research Institute of Bioscience and Biotechnology
    08/28/20
  63. Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.EBI
    Bioorg Med Chem 17: 5139-45 (2009)
    National Human Genome Research Institute
    08/27/20
  64. SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.EBI
    Bioorg Med Chem Lett 20: 1873-6 (2010)
    Korea Research Institute of Bioscience and Biotechnology
    08/27/20
  65. New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.EBI
    Bioorg Med Chem Lett 19: 2722-7 (2009)
    Kyoto Pharmaceutical University
    08/27/20
  66. Novel small-molecule inhibitors of transmissible gastroenteritis virus.EBI
    Antimicrob Agents Chemother 51: 3924-31 (2007)
    National Health Research Institute
    08/27/20
  67. Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors.EBI
    Bioorg Med Chem Lett 17: 5876-80 (2007)
    Purdue University
    08/24/20
  68. Structure-guided design of potent and permeable inhibitors of MERS coronavirus 3CL protease that utilize a piperidine moiety as a novel design element.EBI
    Eur J Med Chem 150: 334-346 (2018)
    Wichita State University
    08/16/20
  69. Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors.EBI
    Bioorg Med Chem 24: 3035-3042 (2016)
    Academia Sinica
    09/14/17
  70. Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.BDB
    J Enzyme Inhib Med Chem 29: 59-63 (2014)
    Gyeongsang National University
    08/28/17
  71. Inhibitor recognition specificity of MERS-CoV papain-like protease may differ from that of SARS-CoV.BDB
    ACS Chem Biol 10: 1456-65 (2015)
    University of Illinois at Chicago
    10/15/15
  72. Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid- hydrolysis.EBI
    Eur J Med Chem 79: 184-93 (2014)
    University of Lille
    02/07/15
  73. Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.EBI
    Bioorg Med Chem Lett 18: 732-7 (2008)
    GlaxoSmithKline
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  74. Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases.EBI
    Bioorg Med Chem 20: 5928-35 (2012)
    Korea Research Institute of Bioscience and Biotechnology
    05/17/13
  75. Structural basis of inhibition specificities of 3C and 3C-like proteases by zinc-coordinating and peptidomimetic compounds.BDB
    J Biol Chem 284: 7646-55 (2009)
    National Yang-Ming University
    10/29/12
  76. Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.EBI
    Bioorg Med Chem Lett 21: 4860-4 (2011)
    Philipps University Marburg
    03/23/12
  77. Virtual screening identification of novel severe acute respiratory syndrome 3C-like protease inhibitors and in vitro confirmation.EBI
    Bioorg Med Chem Lett 21: 3088-91 (2011)
    Chonnam National University
    12/04/11
  78. Stable benzotriazole esters as mechanism-based inactivators of the severe acute respiratory syndrome 3CL protease.BDB
    Chem Biol 13: 261-8 (2006)
    Academia Sinica
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  79. Phage-encoded combinatorial chemical libraries based on bicyclic peptides.EBI
    Nat Chem Biol 5: 502-7 (2009)
    Laboratory of Molecular Biology, Medical Research Council
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  80. Investigation of the pharmacophore space of Severe Acute Respiratory Syndrome coronavirus (SARS-CoV) NTPase/helicase by dihydroxychromone derivatives.EBI
    Bioorg Med Chem Lett 19: 4538-41 (2009)
    Konkuk University
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  81. Aryl diketoacids (ADK) selectively inhibit duplex DNA-unwinding activity of SARS coronavirus NTPase/helicase.EBI
    Bioorg Med Chem Lett 19: 1636-8 (2009)
    Konkuk University
    01/11/10
  82. Thiol-based angiotensin-converting enzyme 2 inhibitors: P1' modifications for the exploration of the S1' subsite.EBI
    Bioorg Med Chem Lett 18: 1681-7 (2008)
    GlaxoSmithKline
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  83. Design and synthesis of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease inhibitors.EBI
    J Med Chem 48: 6767-71 (2005)
    Purdue University
    11/10/09
  84. Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters.EBI
    J Med Chem 50: 1850-64 (2007)
    University of Alberta
    11/10/09
  85. Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.EBI
    J Med Chem 49: 3440-3 (2006)
    Peking University
    11/10/09
  86. Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.EBI
    Bioorg Med Chem Lett 15: 3058-62 (2005)
    Development Center for Biotechnology
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    J Med Chem 52: 5228-40 (2009)
    Purdue University
    09/14/09
  88. Structure-based virtual screening against SARS-3CL(pro) to identify novel non-peptidic hits.BDB
    Bioorg Med Chem 16: 4138-49 (2008)
    University of Mississippi
    07/08/08
  89. Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies.BDB
    J Med Chem 49: 3485-95 (2006)
    National Tsing Hua University
    09/26/06
  90. Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic alpha,beta-unsaturated esters.BDB
    Bioorg Med Chem 13: 5240-52 (2005)
    National Taiwan University
    09/26/06
  91. Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease.BDB
    J Med Chem 49: 5154-61 (2006)
    National Defense Medical Center
    09/26/06
  92. Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.BDB
    J Med Chem 48: 4469-73 (2005)
    National Taiwan University
    09/26/06
  93. Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.BDB
    J Med Chem 49: 4971-80 (2006)
    TaiGen Biotechnology Co.
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BDB Curated by BindingDB
ChEMBL Curated by ChEBML