Home Microbiology Reverse Transcriptase inhibitor Lamivudine

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Lamivudine Reverse Transcriptase inhibitor

Cat.No.S1706

Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase.
Lamivudine Reverse Transcriptase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 229.26

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Quality Control

Batch: Purity: 99.94%
99.94

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT-4 Function assay Concentration required to inhibit syntica formation by 50% in HIV-1 infected MT-4 cells, IC50=0.1μM 8035429
PBMC Function assay Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV, EC50=0.0018μM 8410975
PBMC Function assay Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV, EC50=0.21μM 8410975
PBMC Anti-HIV-1 assay Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.0018μM 8423591
PBMC Anti-HIV-1 assay Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.06μM 8423591
PBMC Anti-HIV-1 assay Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.21μM 8423591
PBMC Anti-HIV-1 assay Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=10.1μM 8423591
2.2.15 Function assay In vitro effective concentration against hepatitis B virus was determined in 2.2.15 cells, EC50=0.008μM 9301659
PBMC Anti-HIV-1 assay In vitro anti-HIV activity in peripheral blood mononuclear cells, EC50=0.07μM 9301659
2.2.15 Antiviral assay Antiviral activity against Hepatitis B virus (HBV) in 2.2.15 cells, EC50=0.008μM 11052795
PBMC Antiviral assay Antiviral activity against Immunodeficiency virus type-1 (HIV-1) in peripheral blood mononuclear cells, EC50=0.07μM 11052795
H9 Antiviral assay Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique, EC50=0.06μM 11430019
H9 Antiviral assay Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique, EC50=0.06μM 11430019
PBMC Antiviral assay Antiviral activity against HIV-1xxBRU mutant strain in human PBM cells, EC90=0.08μM 12383014
PBMC Function assay Activity against Lamivudine-resistant virus (HIV-1XXBRU) in human PBM cells, expressed as EC50, EC50=0.035μM 12852755
PBMC Function assay In vitro concentration required to inhibit the HIV-1 LA1 replication on PBMCs cell (peripheral blood mononuclear cells), EC50=0.01μM 12852943
PBMC Function assay Effective concentration to inhibit HIV-1 LAI cytopathicity in PBMC cells was determined in vitro, EC50=0.0116μM 14971898
HepG2.2.15 Function assay Effective concentration to inhibit hepatitis B virus cytopathicity in HepG2.2.15 cells was determined in vitro, EC50=0.2μM 14971898
MT-4 Function assay Effective concentration to inhibit HIV-1 IIIB cytopathicity in MT-4 cells was determined in vitro, EC50=0.5μM 14971898
PBMC Antiviral assay Antiviral activity against wild type HIV virus(xxBRU) in Human peripheral blood mononuclear (PBM) cells, EC90=0.08μM 15027854
PBMC Function assay Effective concentration against Wild Type HIV-1 virus in human peripheral blood mononuclear cells, EC50=0.041μM 15189036
CEM-SS Antiviral assay 6 days Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay, ED50=0.36μM 15217281
HOG.R5 Antiviral assay 4 days Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=1.2μM 15217281
2.2.15 Function assay Inhibition of HBV replication in 2.2.15 cells by DNA hybridization assay, EC50=0.02μM 15615545
2.2.15 Function assay Effective concentration required to inhibit hepatitis B virus replication in 2.2.15 cells in DNA hybridization assay, EC50=0.05μM 15634003
PBMC Function assay In vitro effective concentration against Lamivudine resistant wild type HIV-1 in human peripheral blood mononuclear cells, EC50=0.027μM 15916425
PBMC Function assay In vitro effective concentration against Lamivudine resistant wild type HIV-1 in human peripheral blood mononuclear cells, EC90=0.25μM 15916425
2.2.15 Function assay Effective concentrations at which 2-fold depression of extracellular virion DNA (HBV) was observed in 2.2.15 Cells, EC50=0.06μM 16033283
2.2.15 Function assay Effective concentrations at which 2-fold depression of extracellular virion DNA (HBV) was observed in 2.2.15 Cells, EC90=0.17μM 16033283
2.2.15 Function assay Effective concentrations at which 10-fold depression of intracellular intermediates of HBV DNA was observed in 2.2.15 Cells, EC50=0.23μM 16033283
2.2.15 Function assay Effective concentrations at which 10-fold depression of intracellular intermediates of HBV DNA was observed in 2.2.15 Cells, EC90=0.69μM 16033283
2.2.15 Function assay Inhibition of synthesis of extracellular virion DNA release in cultured human hepatoblastoma 2.2.15 cells, EC50=0.048μM 16213713
2.2.15 Function assay Inhibition of synthesis of extracellular virion DNA release in cultured human hepatoblastoma 2.2.15 cells, EC90=0.151μM 16213713
2.2.15 Function assay Inhibition of synthesis of intracellular HBV DNA replicative intermediates in cultured human hepatoblastoma 2.2.15 cells, EC50=0.251μM 16213713
2.2.15 Function assay Inhibition of synthesis of intracellular HBV DNA replicative intermediates in cultured human hepatoblastoma 2.2.15 cells, EC90=0.648μM 16213713
2.2.15 Function assay Inhibition of wild type HBV transfected in human hepatoblastoma 2.2.15 cells, EC50=2.1μM 16539393
hepatoma 2.2.15 Antiviral assay Antiviral activity against wild type HBV in human hepatoma 2.2.15 cells, EC50=2.1μM 16759112
2.2.15 Function assay Inhibition of HBV replication in 2.2.15 cells by DNA hybridization assay, EC50=0.02μM 17004726
MDCK2 Function assay 10 uM Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay 17172311
MDCK2 Function assay 10 uM Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay 17172311
MDCK2 Function assay 10 uM Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay 17172311
Huh7 Function assay Inhibition of wild type HBV replication in Huh7 cells, EC50=1μM 17371827
PBMC Antiviral assay Antiviral activity against HIV1 LAI in human PBM cells, EC50=0.026μM 17403996
PBMC Antiviral assay Antiviral activity against HIV1 LAI in human PBM cells, EC90=0.12μM 17403996
HepG2.2.15 Antiviral assay Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR, EC50=0.1μM 17404006
Huh7 Antiviral assay 5 days Antiviral activity against HBV genotype D with reverse transcriptase L80I mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.03μM 17438047
Huh7 Antiviral assay 5 days Antiviral activity against HBeAg-deficient HBV genotype D with precore G1896A mutation and reverse transcriptase L80I mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.03μM 17438047
Huh7 Antiviral assay 5 days Antiviral activity against HBV genotype D in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.41μM 17438047
Huh7 Antiviral assay 5 days Antiviral activity against HBeAg-deficient HBV genotype D with precore G1896A mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.46μM 17438047
HepG2(2.2.15) Antiviral assay Antiviral activity against HBV in ayw wild type HepG2(2.2.15) cells assessed as inhibition of viral DNA replication, IC50=0.05μM 17488817
HepG2(2.2.15) Function assay Inhibition of HBV promoter in human HepG2(2.2.15) cells by luciferase reporter gene assay, IC50=0.08μM 17488817
HepW10 Antiviral assay Antiviral activity against HBV in adriamycin-resistant wild type HepW10 cells assessed as inhibition of viral DNA replication, IC50=0.1μM 17488817
HBV-Met Antiviral assay Antiviral activity against HBV in mouse ayw wild type HBV-Met cells assessed as inhibition of viral DNA replication, IC50=0.2μM 17488817
HepG2.2.15 Function assay 8 days Inhibition of cytoplasmic HBV DNA synthesis in HepG2.2.15 cells after 8 days, IC50=0.38μM 17499889
PBMC Function assay 300 mg 7 days Cmax in HIV-infected human assessed as Lamivudine monophosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000008μM 17664328
PBMC Function assay 300 mg 7 days Cmax in HIV-infected human assessed as Lamivudine diphosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000044μM 17664328
PBMC Function assay 300 mg 7 days Cmax in HIV-infected human assessed as Lamivudine triphosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000048μM 17664328
MAGIC-5A Antiviral assay 40 hrs Antiviral activity against wild type HIV1 NL4-3 produced from full length pR9deltaApa infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=0.88μM 17967913
MAGIC-5A Antiviral assay 40 hrs Antiviral activity against wild type HIV2 ROD produced from full length pROD9 infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=2μM 17967913
MAGIC-5A Antiviral assay 40 hrs Antiviral activity against multinucleoside-resistant HIV1 NL4-3 harboring A62V, V75I, F77L, F116Y, Q151M mutation in viral reverse transcriptase infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=3.7μM 17967913
PBMC Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.04μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.04μM 18316521
MT2 Antiviral assay Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells, EC50=0.04μM 18316521
MT2 Antiviral assay Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.047μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.063μM 18316521
PBMC Antiviral assay Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.071μM 18316521
PBMC Antiviral assay Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.081μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.086μM 18316521
MT2 Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.105μM 18316521
MT2 Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.171μM 18316521
MT2 Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.182μM 18316521
MT2 Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.183μM 18316521
MT2 Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.202μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.219μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.372μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=0.462μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.554μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=0.667μM 18316521
PBMC Antiviral assay 1 hr Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.85μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.927μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.969μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay, EC50=1.14μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=1.259μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=1.683μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=1.985μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=2.445μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=2.47μM 18316521
MT2 Antiviral assay 5 days Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=3.247μM 18316521
HepG2(2.2.15) Antiviral assay 24 hrs Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as extracellular HBV virion DNA level after 24 hrs, EC50=0.048μM 19072694
HepG2(2.2.15) Antiviral assay 24 hrs Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as replication intermediates after 24 hrs, EC50=0.15μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against lamivudine-resistant wild type HBV in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=0.2μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against lamivudine-resistant HBV reverse transcriptase 236T mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=0.3μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against adefovir-resistant wild type HBV in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.3μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against adefovir-resistant HBV reverse transcriptase M204V mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.5μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against adefovir-resistant HBV reverse transcriptase L180M mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.6μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against adefovir-resistant HBV reverse transcriptase LM/reverse transcriptase MV double mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.6μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against adefovir-resistant HBV reverse transcriptase M204I mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.8μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against adefovir-resistant HBV reverse transcriptase 236T mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=7.7μM 19072694
Huh7 Antiviral assay 4 days Antiviral activity against lamivudine-resistant HBV reverse transcriptase L180M mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=10μM 19072694
HuH7 Antiviral assay 24 hrs Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=0.2μM 19398648
HuH7 Antiviral assay 24 hrs Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=0.3μM 19398648
HuH7 Antiviral assay 24 hrs Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=1.5μM 19398648
HuH7 Antiviral assay 24 hrs Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=3μM 19398648
HuH7 Antiviral assay 24 hrs Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=16μM 19398648
HuH7 Antiviral assay 24 hrs Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=41μM 19398648
MT2 Antiviral assay Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.6μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=0.78μM 19596885
TZM-bl Antiviral assay 72 hrs Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=0.47μM 19704131
TZM-bl Antiviral assay Antiviral activity against wild-type HIV1 pNL4-3 infected in TZM-bl cells by luciferase assay, EC50=0.65μM 19704131
TZM-bl Antiviral assay 72 hrs Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=1.08μM 19704131
TZM-bl Antiviral assay 72 hrs Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S/T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=2.1μM 19704131
HepG2.2.15 Antiviral assay Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA replication, IC50=0.22μM 19897363
1.3ES2 Antiviral assay 6 days Antiviral activity against Hepatitis B virus ayw in human 1.3ES2 cells stably transfected with 1.3 fold wild type HBV ayw strain genome cells assessed as reduction of viral DNA level after 6 days by RT-PCR 20061158
HepG2.2.15 Antiviral assay 9 days Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=0.2μM 20117930
HepG2.2.15 Antiviral assay 9 days Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=0.2μM 20117930
HepG2.2.15 Antiviral assay 9 days Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=0.7μM 20117930
HepG2.2.15 Antiviral assay 9 days Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=0.8μM 20117930
HepG2.2.15 Antiviral assay 9 days Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=5.3μM 20117930
HepG2.2.15 Antiviral assay 9 days Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=20μM 20117930
HepG2(2.2.15) Antiviral assay 13 uM 72 hrs Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA level at 13 uM after 72 hrs by RT-PCR analysis 20176893
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.25μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.54μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.9μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.06μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.24μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.48μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.68μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.78μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=5.43μM 20308377
HEK293 Antiviral assay 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=7.16μM 20308377
HepG2(2.2.15) Antiviral assay 8 days Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral cytoplasmic DNA synthesis after 8 days by RT-PCR analysis, IC50=0.16μM 20639110
HepG2(2.2.15) Cytotoxicity assay 8 days Cytotoxicity against human HepG2(2.2.15) cells after 8 days by MTT assay, CC50=5μM 20639110
MT2 Antiviral assay 2 to 3 days Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR, EC50=0.8μM 21115794
MT2 Antiviral assay Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V, M184I mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysis, EC50=0.8μM 21115794
MT2 Antiviral assay Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysis, EC50=0.8μM 21115794
MT2 Antiviral assay Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V, M184I, K82N mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysi, EC50=0.8μM 21115794
HepG2(2.2.15) Antiviral assay Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in viral DNA by Southern blotting, EC50=0.06μM 21333535
Huh7 Antiviral assay 1 day Antiviral activity against Hepatitis B virus infected in human Huh7 cells assessed as reduction in viral DNA after 1 day by Southern blotting, EC50=0.1μM 21333535
HuH7 Cytotoxicity assay 4 days Cytotoxicity against human HuH7 cells after 4 days by neutral red dye uptake assay, CC50=0.1μM 21333535
HepG2(2.2.15) Antiviral assay 4 days Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 4 days by RT-PCR analysis, IC50=0.33μM 21524588
HepG2(2.2.15) Antiviral assay 9 days Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method, EC50=0.2μM 21930377
HepG2(2.2.15) Antiviral assay 9 days Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization meth, EC50=0.2μM 21930377
HepG2(2.2.15) Antiviral assay 9 days Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybridization assay, EC90=0.6μM 21930377
HepG2(2.2.15) Antiviral assay 9 days Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybri, EC90=0.9μM 21930377
HepG2(2.2.15) Antiviral assay 9 days Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization me, EC50=1.5μM 21930377
HepG2(2.2.15) Antiviral assay 9 days Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hyb, EC90=22μM 21930377
HeLa P4/R5 Antiviral assay 2 hrs Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay, EC50=11.3μM 22352809
HeLa P4/R5 Antiviral assay 2 hrs Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay, EC50=32.7μM 22352809
HeLa P4/R5 Antiviral assay 2 hrs Antiviral activity against HIV1 BaL assessed as inhibition of infection in HeLa P4/R5 cells expressing CD4 receptor and beta-gal incubated for 2 hrs followed by compound-wash out measured after 46 hrs by single round infection MAGI assay, EC50=11.4μM 22533850
HeLa P4/R5 Antiviral assay 2 hrs Antiviral activity against HIV1 3B assessed as inhibition of infection in HeLa P4/R5 cells expressing CD4 receptor and beta-gal incubated for 2 hrs followed by compound-wash out measured after 46 hrs by single round infection MAGI assay, EC50=32.7μM 22533850
CEM-SS Antiviral assay 6 days Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay, EC50=0.2μM 22858097
HuH7 Antiviral assay Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells, EC50=0.056μM 23237841
HuH7 Antiviral assay Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells, EC90=0.142μM 23237841
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay, EC50=1.8μM 24119448
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay, EC50=5.9μM 24119448
CEM Antiviral assay 4 days Antiviral activity against HIV1 3B infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis, EC50=0.099μM 24177359
CEM Antiviral assay 4 days Antiviral activity against HIV2 ROD infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis, EC50=0.18μM 24177359
HOG.R5 Antiviral assay Antiviral activity against HIV-1 3B/H9 infected in human HOG.R5 cells transfected with HIV1 LTR-GFP assessed as inhibition of viral replication by fluorescence analysis, IC50=1.2μM 24404757
MT4 Antiviral assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay, EC50=2.442μM 24794751
MT4 Antiviral assay Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay, EC50=7.2μM 24794751
MT4 Antiviral assay 5 days Antiviral activity against Human immunodeficiency virus 1 3b infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay, IC50=3.9μM 24926807
MT4 Antiviral assay 5 days Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay, IC50=15.5μM 24926807
MT4 Antiviral assay 5 days Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, IC50=3.89μM 24952305
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, IC50=15.53μM 24952305
HepG2.2.15 Antiviral assay Antiviral activity against hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of viral replication, IC50=14.17μM 25127104
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay, EC50=2.22μM 25240095
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay, EC50=8.81μM 25240095
HepG2(2.2.15) Function assay 0.75 to 3 uM 72 hrs Decrease in HBV viral DNA replication in human HepG2(2.2.15) cells at 0.75 to 3 uM after 72 hrs by real-time PCR analysis, IC50=7.63μM 25461891
MT4 Antiviral assay 5 days Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.24μM 25537532
MT4 Antiviral assay 5 days Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay, EC50=8.79μM 25537532
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.239μM 25626145
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay, EC50=0.89μM 25682562
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay, EC50=3.56μM 25682562
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.2μM 25707013
HepG2.2.15 Antiviral assay Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of HBV DNA replication by real-time fluorescence quantitative PCR analysis, IC50=6.86μM 25847765
MT4 Antiviral assay 5 days Antiviral activity against HIV1-3B infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay, EC50=3.9μM 25946116
MT4 Antiviral assay 5 days Antiviral activity against HIV2-ROD infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay, EC50=15.5μM 25946116
HepG22.2.15 Antiviral assay 3 days Antiviral activity against HBV infected in human HepG22.2.15 cells after 3 days by neutral red dye-based plaque reduction assay, IC50=0.039μM 26260336
U87 Antiviral assay 10 uM 4 days Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 10 uM measured after 4 days by p24 ELISA 27091070
U87 Antiviral assay 100 uM 4 days Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 100 uM measured after 4 days by p24 ELISA 27091070
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=3.1μM 27267005
HepG2.2.15.7 Antiviral assay 9 days Antiviral activity against HBV infected in human HepG2.2.15.7 cells assessed as inhibition of viral DNA level after 9 days by real time PCR method, EC50=0.03μM 27426303
MT4 Antiviral assay 5 days Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay, EC50=2.24μM 27541578
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay, EC50=8.79μM 27541578
HepG2(2.2.15) Antiviral assay 6 days Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days by real-time qPCR method, EC50<0.01μM 27748590
HepG2(2.2.15) Antiviral assay 6 days Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method, EC50=0.01μM 27748590
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.22μM 27748590
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=8.81μM 27748590
Huh7 Antiviral assay Antiviral activity against lamivudine-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in secreted DNA levels measured on day 7 by real-time PCR analysis, EC50=0.055μM 28082068
HepG2.215 Antiviral assay Antiviral activity against hepatitis B virus infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis, EC50=0.1μM 28082068
Huh7 Antiviral assay Antiviral activity against lamivudine-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in intracellular DNA levels measured on day 7 by real-time PCR analysis, EC50=0.237μM 28082068
HepG2.215 Antiviral assay Antiviral activity against hepatitis B virus infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis, EC90=2μM 28082068
HepAD38 Antiviral assay 5 days Antiviral activity against HBV infected in human HepAD38 cells assessed as inhibition of DNA replication after 5 days by RT-PCR method, EC50=0.04μM 28094179
P4R5 MAGI Function assay 2 hrs Inhibition of HIV1 BaL dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay, EC50=11.3μM 28351588
P4R5 MAGI Function assay 2 hrs Inhibition of HIV1 3B dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay, EC50=32.7μM 28351588
HepG2.2.15 Antiviral assay 8 days Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of viral DNA replication after 8 days by real time fluorescent PCR method, IC50=0.5μM 28494252
MT4 Antiviral assay 5 days Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.54μM 28659246
HepG2(2.2.15) Antiviral assay 6 days Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days byr by real-time qPCR assay, EC50=0.00887μM 28682067
HepG2(2.2.15) Antiviral assay 6 days Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method, EC50=0.02μM 28682067
HepAD38 Antiviral assay Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method, EC50<0.01μM 28688280
HepAD38 Antiviral assay Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral replication by RT-PCR method, EC50=0.04μM 28688280
HepAD38 Antiviral assay Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method, EC50=0.04μM 28688280
HepAD38 Antiviral assay Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral replication by RT-PCR method, EC90=0.3μM 28688280
HepAD38 Antiviral assay Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method, EC90=0.3μM 28688280
HepAD38 Antiviral assay Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method, EC90=0.7μM 28688280
SupT1 Antiviral assay 48 hrs Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay, IC50=0.1μM 29016131
HepG2(2.2.15) Antiviral assay 6 days Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 6 days by RT-PCR method, IC50<0.1μM 29288943
A549 Antiviral assay Antiviral activity against HIV1 virions derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-mixed virions followed by incubation with target cel, IC50=0.51μM 29699924
HepG2.2.15 Antiviral assay 6 days Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction in extracellular viral DNA levels after 6 days by qPCR/TaqMan assay, IC50=0.025μM 30286292
MT4 Antiviral assay 5 days Antiviral activity against HIV1 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=7.77μM 30606670
MT4 Antiviral assay 5 days Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=12.8μM 30606670
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay, EC50=6.41μM 30721060
HepG2.2.15 Function assay 4 uM 6 days Inhibition of capsid protein in Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction in viral DNA level at 4 uM supplemented with fresh medium containing compound every 2 days and measured after 6 days by RT-PCR analysis, IC50<0.1μM 31091479
HepG2.2.15 Antiviral assay Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=2.22μM 31223460
C8166 Antiviral assay 72 hrs Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of syncytial cell formation incubated for 72 hrs, EC50=0.3μM 31310115
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=1.92μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.14μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.58μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.7μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.88μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=4.45μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=4.54μM 31434039
MT4 Antiviral assay 5 days Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=5.54μM 31434039
PBMC Antiviral assay Antiviral activity in PBM cells expressed as IC50, IC50=0.002μM ChEMBL
HepG2.2.15 Antiviral assay Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells), EC50=0.01μM ChEMBL
HepG2.2.15 Function assay Effective concentration necessary to decrease extracellular Hepatitis B virus DNA levels by 50% in human hepatoblastoma cell line (2.2.15 cells) in vitro, EC50=0.038μM ChEMBL
PBMC Function assay Compound was tested for its anti-HIV activity against HIV-1 LAI in human peripheral blood mononuclear (PBM) cells, EC50=0.06μM ChEMBL
HepG2.2.15 Function assay Effective concentration necessary to decrease extracellular Hepatitis B virus DNA levels by 90% in human hepatoblastoma cell line (2.2.15 cells) in vitro, EC90=0.16μM ChEMBL
HepG2.2.15 Function assay Tested for the effective concentration required to inhibit HBV in HepG2.2.15 human liver cells, EC50=0.2μM ChEMBL
PBMC Antiviral assay Antiviral activity in PBM cells, IC50=0.21μM ChEMBL
PBMC Antiviral assay Antiviral activity in PBM cells expressed as IC50, IC50=0.21μM ChEMBL
MT-4 Antiviral assay Antiviral activity in MT-4 cells, IC50=0.37μM ChEMBL
MT-4 Antiviral assay Antiviral activity in MT-4 cells expressed as IC50, IC50=0.37μM ChEMBL
MT-4 Antiviral assay Antiviral activity in MT-4 cells expressed as IC50, IC50=0.61μM ChEMBL
MT-4 Function assay Compound was tested for its anti-HIV activity in acutely infected MT-4 cells, EC50=7μM ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 45 mg/mL (196.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 45 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 229.26 Formula

C8H11N3O3S

 Storage (From the date of receipt)
CAS No. 134678-17-4 Download SDF Storage of Stock Solutions

Synonyms GR109714X, BCH-189 Smiles C1C(OC(S1)CO)N2C=CC(=NC2=O)N

Mechanism of Action

Targets/IC50/Ki
Reverse transcriptase
In vitro

Lamivudine’s anti- HBV activity, like its anti-HIV activity, has been shown to depend on the ability of LMV-TP to serve as both substrate and inhibitor of the DNA- and RNA-dependent polymerase activities of the HBV P gene product. This compound owes its activity to the remarkably broad substrate specificity of deoxycytidine kinase and the unusual substrate preference of the HBV polymerases for dNTPs with the unnatural L-conformation, whereas the anti-HBV activity of PCV appears to depend on several factors including optimal phosphorylation (sufficient for antiviral activity but not cytotoxicity) by key cellular enzymes, the long intracellular half-life of PCV-TP and the ability of PCV-TP to inhibit the HBV RT priming reaction as well as RT and DNA polymerase activity.

This compound and Penciclovir inhibits duck hepatitis B virus (DHBV) replication to a comparable extent when used alone, and in combination, the two nucleoside analogs acts synergistically over a wide range of clinically relevant concentrations. It combined with Penciclovir is more effective in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV than either drug alone.

It inhibits p24 antigen production by HIV-I in PBMC, with ED50s ranging from 0.07 μM to 0.2 μM.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/33898535/
  • [5] https://www.sciencedirect.com/science/article/pii/S1818087616000131

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06056596 Recruiting
Retinal Detachment|Rhegmatogenous Retinal Detachment
University of Wisconsin Madison
 January 30 2024 Early Phase 1
NCT04133012 Completed
HIV-1 Infection
ANRS Emerging Infectious Diseases|ViiV Healthcare
 February 10 2020 Not Applicable

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