Assay ID | Title | Year | Journal | Article |
AID1803988 | FRET protease activity assay from Article 10.1101/2020.09.12.293498: \\Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19.\\ | | | |
AID1805532 | Various Assay from Article 10.1002/cmdc.202100576: \\A patent review on SARS coronavirus main protease (3CLpro) inhibitors.\\ | 2022 | ChemMedChem, 01-05, Volume: 17, Issue:1
| A Patent Review on SARS Coronavirus Main Protease (3CL |
AID1805143 | Literature assay from Article 10.1016/j.bmcl.2021.128263: \\A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.\\ | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors. |
AID1805744 | FRET-based enzymatic assay from Article 10.1021/jacs.1c08060: \\Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity.\\ | 2021 | Journal of the American Chemical Society, 12-15, Volume: 143, Issue:49
| Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity. |
AID1805142 | fluorescence resonance energy transfer (FRET)-based CoV-2 3CLpro inhibition assay from Article 10.1016/j.bmcl.2021.128263: \\A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.\\ | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors. |
AID1698973 | Cytotoxicity against African green monkey Vero 76 cells measured after 66 hrs by neutral red method or cell titer glo-based luminescence assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857889 | Antiviral activity against HCoV-OC43 infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1897967 | Inhibition of SARS-CoV-2 main protease expressed in Escherichia coli using Dabcyl-KTSAVLQSGFRKME-Edans as substrate incubated for 60 mins by FRET based assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors. |
AID1698932 | Inhibition of human thrombin at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698920 | Half life in dog at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698945 | Antiviral activity against HIV-1-RF infected in human H9 cells assessed as reduction in virus-induced cytopathogenicity incubated for 7 days by XTT dye based analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698944 | Antiviral activity against Human rhinovirus 16 infected in human H1-HeLa cells assessed as reduction in virus-induced cytopathogenicity incubated for 2 to 5 days by XTT dye based analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698930 | Inhibition of human chymotrypsin at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857888 | Antiviral activity against MERS-CoV EMC2012 infected in HEK293T cells transfected with DPP4 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698926 | Inhibition of human cathepsin D at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698960 | Clearance in monkey at 4 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698922 | Inhibition of SARS-CoV-2 3CL protease using DABCYLKTSAVLQ-SGFRKME-EDANS as peptide substrate in presence of PF-00835231 inhibitor incubated for 60 mins by FRET assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698953 | Clearance in rat at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698950 | Antiviral activity against Human coronavirus 229E infected in human MRC5 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days in presence of p-glycoprotein inhibitor CP100356 by XTT dye based assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698957 | Clearance in dog at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857887 | Antiviral activity against SARS CoV infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1897968 | Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24
| Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors. |
AID1698927 | Inhibition of human leukocyte elastase | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1821845 | Inhibition of SARS-CoV-2 3CL protease | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CL |
AID1698928 | Inhibition of human leukocyte elastase at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857901 | Inhibition of SARS-CoV-2 3CLpro spiked in human A-431 cells assessed as decrease in fluorescence intensity at 0.5 uM incubated for 30 mins in presence of N-((S)-1-{2-[(R)-2-Chloro-2-fluoroacetyl]-2-{[(S)-2-oxopyrrolidin-3-yl]methyl}hydrazineyl}-4-methyl-1 | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1857886 | Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698946 | Antiviral activity against Hepatitis C virus replicon infected in human Huh-7 cells assessed as reduction in viral RNA synthesis measured after 24 to 72 hrs by Trizol reagent based RT-PCR analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698940 | Inhibition of HCV protease at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698924 | Inhibition of human cathepsin B at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698958 | Volume of distribution at steady state in dog at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698970 | Cytotoxicity against human H9 cells assessed as reduction in cell viability incubated for 7 days by XTT dye based analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698966 | Aqueous solubility of compound in 2.5% w/v HPCD formulation | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698941 | Inhibition of HRV protease | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698939 | Inhibition of HCV protease | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698937 | Inhibition of HIV1 protease | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1851890 | Inhibition of human Cathepsin L using Z-Leu-Arg-AMC as fluorogenic substrate incubated for 60 mins by FRET assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity. |
AID1857878 | Antiviral activity against wild type SARS CoV-2 infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698969 | Cytotoxicity against human H1-HeLa cells assessed as reduction in cell viability measured after 2 to 5 days by XTT assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698925 | Inhibition of human cathepsin D | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698967 | Inhibition of Human coronavirus 229E protease | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698935 | Inhibition of human Caspase 2 | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698938 | Inhibition of HIV1 protease at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698934 | Inhibition of human pepsin at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698972 | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 1 to 5 days by XTT dye based assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857879 | Antiviral activity against SARS CoV-2 alpha QK002 infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698915 | Antiviral activity against SARS COV-1 infected in monkey vero 76 cells assessed as reduction in virus-induced cytopathic effect measured after 66 hrs by neutral red method or cell titer glo-based luminescence assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698962 | Half-life in monkey at 4 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857869 | Inhibition of recombinant full length SARS-CoV-2 3CLpro expressed in Escherichia coli using Ac-Abu-Tle-Leu-Gln-MCA as fluorogenic substrate preincubated for 30 mins followed by substrate addition and measured for 6 hrs by multimode plate reader analysis | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698948 | Selectivity index, ratio of EC50 for antiviral activity against SARS COV-1 infected in monkey vero 76 cells to EC50 for antiviral activity against Human coronavirus 229E infected in human MRC5 cells | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698949 | Antiviral activity against SARS COV-1 infected in monkey Vero 76 cells assessed as reduction in virus-induced cytopathic effect measured after 66 hrs in presence of p-glycoprotein inhibitor CP100356 by neutral red method or cell titer glo-based luminescen | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1751777 | Inhibition of SARS coronavirus 1 3CL protease expressed in Escherichia coli measured by HPLC method | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors. |
AID1851889 | Inhibition of SARS-CoV-2 main protease using MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 as fluorescent substrate preincubated for 10 mins followed by substrate addition and measured every 10 sec for 10 mins by FRET assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity. |
AID1698942 | Antiviral activity against Human coronavirus 229E infected in human MRC5 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by XTT dye based assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698954 | Volume of distribution at steady state in rat at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857881 | Antiviral activity against SARS CoV-2 omicron TY38-873 BA.1 variant infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1857882 | Antiviral activity against SARS CoV-2 omicron TY38-873 BA.2 variant infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1871194 | Inhibition of SARS-CoV-2 3CL protease by FRET assay | 2021 | RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
| Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors. |
AID1698971 | Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698929 | Inhibition of human chymotrypsin | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698936 | Inhibition of human Caspase 2 at 10 uM relative to control | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698931 | Inhibition of human thrombin | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857884 | Antiviral activity against wild type SARS CoV-2 infected in Vero E6 cells transfected with TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698955 | Half-life in rat at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857880 | Antiviral activity against SARS CoV-2 delta TY11-927 infected in HEK293T cells transfected with ACE2 and TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1857883 | Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698956 | AUC in rat at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698933 | Inhibition of human pepsin | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698961 | Volume of distribution at steady state in monkey at 4 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698963 | AUC in monkey at 4 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1751770 | Inhibition of SARS-CoV-2 3CLpro preincubated for 30 mins followed by addition of (Dabcyl)KTSAVLQSGFRKM(Glu) peptide substrate and measured after 1.5 hrs by FRET assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors. |
AID1698918 | Reversible inhibition of SARS coronavirus Urbani 3CL protease(9985 to 10902) using TAMRA-SITSAVLQSGFRKMK(DABCYL)-OH as substrate measured for 10 mins by FRET assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698923 | Inhibition of human cathepsin B | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698921 | Metabolic stability in human liver microsomes assessed as half life | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698952 | Aqueous solubility of compound in 2.5% w/v SBECD, pH 7.4 5 mM citrate buffer, made isotonic with 4.25% dextrose formulation | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698951 | Aqueous solubility of compound in 2.5% w/v SBECD, pH 7.4 5 mM phosphate buffer, made isotonic with 4.25% dextrose formulation | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1851893 | Inhibition of human Cathepsin B using Z-Leu-Arg-AMC as fluorogenic substrate incubated for 60 mins by FRET assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity. |
AID1698959 | AUC in dog at 2 mg/kg, iv | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698919 | Permeability of compound in human Caco-2 cells | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698968 | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 4 days by XTT dye based assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1698943 | Antiviral activity against Human rhinovirus 14 infected in human H1-HeLa cells assessed as reduction in virus-induced cytopathogenicity incubated for 2 to 5 days by XTT dye based analysis | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
AID1857885 | Antiviral activity against wild type SARS CoV-2 infected in Vero E6 cells transfected with TMPRSS2 assessed as inhibition of virus induced cytopathic effect incubated for 2 to 3 days in presence of P-gp inhibitor CP-100356 by MTT assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease. |
AID1698947 | Antiviral activity against Human cytomegalovirus AD169 infected in human MRC5 cells assessed as reduction in viral replication measured after 5 days by ELISA | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |