Stability in human liver microsomes assessed as compound remaining level incubated for 60 mins in presence of NADPH regenerating system by LC-MS/MS analysis
Inhibition of purified recombinant HIV1 reverse transcriptase assessed as remaining enzyme activity at 0.2 uM using template/primer hybrid, digoxigenin-labeled nucleotides and biotin-labeled nucleotides incubated for 1 hr by calorimetric assay relative to control
Potency index, ratio of IC50 for PF-74 to IC50 for test compound for antiviral activity against HIV1 Env-pseudotyped virus in human U87.CD4.CCR5 target cells assessed as reduction in viral infection at early stage
Selectivity index, ratio of IC50 for antiviral activity against HIV1 Env-pseudotyped virus in human U87.CD4.CCR5 target cells assessed as reduction in viral infection at late stage to IC50 for antiviral activity against HIV1 Env-pseudotyped virus in human U87.CD4.CCR5 target cells assessed as reduction in viral infection at early stage
Selectivity index, ratio of Kd for binding affinity to HIV1 NL4-3 capsid protein monomer by SPR analysis to Kd for binding affinity to HIV1 NL4-3 capsid protein hexamer by SPR analysis
Selectivity index, ratio of CC50 for cytotoxicity in human TZM-bl assessed as reduction in cell viability incubated for 1 day by Cyto-tox-Glo cytotoxicity assay to EC50 for antiviral activity against HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in virus induced cytopathogenicity incubated for 1 day by luciferase reporter gene assay
Antiviral activity against HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in virus induced cytopathogenicity incubated for 1 day by luciferase reporter gene assay