Inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by FRET assay
Inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate at 50 uM preincubated for 15 mins followed by substrate addition and measured after 15 mins by FRET assay relative to control
Inhibition of full length DENV2 NS2B-NS3 protease in human HeLa cells expressing luciferase reporter gene incubated for 24 hrs by luminescence analysis
Inhibition of full length DENV2 NS2B-NS3 protease in human HeLa cells expressing luciferase reporter gene at 12.5 uM incubated for 24 hrs by luminescence analysis relative to control
Cytotoxicity against human HeLa cells expressing luciferase-based DENV-2 protease reporter system assessed as reduction in cell viability by celltiter-blue assay
Potency index, ratio of boceprevir IC50 to test compound IC50 for inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by FRET assay
Competitive inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) using varying concentrations of 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by Cheng-prusoff equation analysis
Mixed-type inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) assessed as decrease in Vmax with constant Km using varying concentrations of 2-Abz-Ser-AlaVal-Leu-Gln-Ser-Gly-Tyr(3-NO2)-Arg-OH as substrate by Michaelis-Menten analysis
Inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) assessed as inhibition constant by Michaelis-Menten analysis
Time dependent inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) at 12.5 uM measured upto 60 mins
Reversible inhibition of C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) at 100 uM preincubated for 2 hrs followed by dilution to 3 uM and substrate addition measured after 15 mins by fluorimetric assay
Binding affinity to C-terminal His tagged SARS CoV-2 main protease transfected in Escherichia coli BL21 (DE3) assessed as covalent bond formation by measuring mass adduct at 100 uM by ESI-TOF analysis
Inhibition of trypsin (unknown origin) using Boc-Val-Pro-Arg-AMC as substrate assessed as enzymatic cleavage at 50 uM preincubated for 15 mins followed by substrate addition and measured after 15 mins by continuous fluorimetric assay
Inhibition of thrombin (unknown origin) using Boc-Val-Pro-Arg-AMC as substrate assessed as enzymatic cleavage at 50 uM preincubated for 15 mins followed by substrate addition and measured after 15 mins by continuous fluorimetric assay
Cytotoxicity against human HeLa cells expressing renilla luciferase reporter construct assessed as reduction in cell viability at 12.5 uM by luciferase based analysis
Antiviral activity against Dengue virus serotype 2 infected in Huh-7 cells assessed as reduction in virus titer at 12.5 uM incubated for 48 hrs followed by infection of Vero E6 cells with supernatant and measured after 7 days by crystal violet staining based analysis relative to control
Chemical stability of the compound in SARS-CoV-2 main protease assay buffer assessed as SARS-CoV-2 main protease-mediated amide bond cleavage at 100 uM measured after 8 hrs by HPLC based UV-Vis analysis