| Assay ID | Title | Year | Journal | Article |
|---|
| AID341863 | Apparent oral clearance in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID1328888 | Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Discovery of 2'-α-C-Methyl-2'-β-C-fluorouridine Phosphoramidate Prodrugs as Inhibitors of Hepatitis C Virus. |
| AID547048 | Antiviral activity against Hepatitis C virus Con1 infected in human lunet cells assessed as inhibition of viral RNA replication after 4 days by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. |
| AID386302 | Drug uptake in human hepatocyte at 50 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386274 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrine-2,4(1H,3H)-trione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342037 | Metabolic stability in human whole blood at 1000 dpm/pmol after 2 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341869 | Drug level in rhesus monkey cerebrospinal fluid at 33.3 mg/kg, iv administered as single dose after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID493450 | Cytotoxicity against human HuH7 cells by MTS assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and anti-HCV activity of 3',4'-oxetane nucleosides. |
| AID341855 | Tmax in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386072 | Drug uptake in human hepatocyte at 2 uM after 48 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID520335 | Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| The hepatitis C virus replicon presents a higher barrier to resistance to nucleoside analogs than to nonnucleoside polymerase or protease inhibitors. |
| AID1191709 | Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors. |
| AID431228 | Ratio of Kcat to Km for cloned cytidine deaminase in human HuH7 cells by spectrophotometric analysis | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID386298 | Drug uptake in human hepatocyte at 250 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341867 | AUMC in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID278937 | Ratio of Kcat to Km for UCK1 activity expressed in Huh7 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. |
| AID386297 | Drug uptake in human hepatocyte at 100 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID431255 | Ratio of EC90 for wild type HCV in viral replicon RNA-containing human HuH7 cells in absence of zedularine to EC90 wild type HCV in viral replicon RNA-containing human HuH7 cells in presence of zedularine | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID547049 | Antiviral activity against Hepatitis C virus isolate Con1 infected in human HuH-7 cells assessed as inhibition of viral RNA replication after 4 days by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. |
| AID1191710 | Inhibition of HCV genotype 1b NS5B RNA dependent RNA polymerase assessed as reduction in triphosphate activity | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors. |
| AID341862 | Apparent oral clearance in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386287 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341852 | Terminal half life in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386290 | Drug uptake in human hepatocyte at 50 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342049 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 2 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386286 | Drug uptake in human hepatocyte at 250 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386294 | Drug uptake in human hepatocyte at 10 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386296 | Drug uptake in human hepatocyte at 50 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386073 | Drug uptake in human hepatocyte at 2 uM after 72 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386304 | Drug uptake in human hepatocyte at 250 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386282 | Drug uptake in human hepatocyte at 10 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386063 | Drug uptake in human hepatocyte at 100 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID536907 | Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase. |
| AID341873 | Mean absorption time in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID1191708 | Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
| Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors. |
| AID342042 | Metabolic stability in human whole blood at 1000 dpm/pmol after 48 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID245981 | Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication. |
| AID386066 | Inhibition of RNA synthesis activity of HSV 1b Con1 NS5B polymerase | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342046 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 0.25 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341868 | AUMC in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386292 | Drug uptake in human hepatocyte at 250 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342054 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 48 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341856 | Cmax in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID278948 | Activity of human UCK1 expressed in Huh7 cells assessed as phosphorylation up to 3 mM by coupled enzyme assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. |
| AID431251 | Antiviral activity against wild type HCV infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay in absence of DCTD inhibitor zedularine | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID246788 | Effective concentration required to reduce HCV replication RNA levels in Huh7 cells by 90% determined by HCV replicon assay | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication. |
| AID386068 | Drug uptake in human hepatocyte at 2 uM after 1 hr assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID1070866 | Inhibition of HCV genotype 1b recombinant NS5B RNA dependent RNA polymerase S282T mutant using IRES RNA as substrate after 30 mins by radioactive assay in presence of [alpha32p]UTP | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
| Use of 2'-spirocyclic ethers in HCV nucleoside design. |
| AID341857 | Cmax in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386285 | Drug uptake in human hepatocyte at 100 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342052 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 10 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341865 | Mean residence time in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID429056 | Metabolic stability in human hepatocytes assessed as RO2433 triphosphate half life at 2 uM | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID342048 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 1 hr at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID429044 | Ratio of Kcat to Km for cloned 2'-deoxycytidine kinase in human HepG2 cells assessed as formation of formation of PS-6130 monophosphate by spectrophotometry | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID386070 | Drug uptake in human hepatocyte at 2 uM after 16 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID245926 | Cytotoxic concentration against bovine viral diarrhea virus (BVDV) in MDBK cells | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication. |
| AID386078 | Drug uptake in human hepatocyte at 2 uM after 72 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID547047 | Half life in human hepatocytes | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. |
| AID493448 | Antiviral activity against HCV 1a infected in human HB-1 cells assessed as inhibition of viral RNA replication after 24 hrs | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and anti-HCV activity of 3',4'-oxetane nucleosides. |
| AID342051 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 8 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386289 | Drug uptake in human hepatocyte at 25 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341851 | Cytotoxicity against human HepG2 cells | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386275 | Drug uptake in human hepatocyte at 2 uM after 48 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrine-2,4(1H,3H)-trione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386062 | Drug uptake in human hepatocyte at 250 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342035 | Metabolic stability in human whole blood at 1000 dpm/pmol after 0.5 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID342038 | Metabolic stability in human whole blood at 1000 dpm/pmol after 4 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID278932 | Activity of human dCK expressed in HepG2 cells assessed as phosphorylation by coupled enzyme assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. |
| AID341854 | Tmax in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID493451 | Activity at human recombinant deoxycytidine kinase expressed in HepG2 cells | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and anti-HCV activity of 3',4'-oxetane nucleosides. |
| AID431227 | Activity of cloned cytidine deaminase in human HuH7 cells at 4 mM by spectrophotometric analysis | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID431252 | Antiviral activity against HCV harboring NS5B polymerase S282T mutation infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay in absence of DCTD inhibitor zedularine | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID386079 | Drug uptake in human hepatocyte at 2 uM after 6 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrine-2,4(1H,3H)-trione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342040 | Metabolic stability in human whole blood at 1000 dpm/pmol after 10 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341875 | Oral bioavailability in rhesus monkey assessed as parent drug plus 2'-deoxy-2'-fluoro-2'-C-methyluridine level at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID520336 | Cytotoxicity against human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| The hepatitis C virus replicon presents a higher barrier to resistance to nucleoside analogs than to nonnucleoside polymerase or protease inhibitors. |
| AID386279 | Drug uptake in human hepatocyte at 25 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341860 | Apparent volume of distribution with respect to bioavailability in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386293 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341850 | Antiviral activity against HCV in human Huh7 cells by replicon based assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID1071246 | Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
| Nucleotide prodrugs of 2'-deoxy-2'-spirooxetane ribonucleosides as novel inhibitors of the HCV NS5B polymerase. |
| AID342050 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 4 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID278950 | Ratio of Kcat to Km for UCK1 activity expressed in Huh7 cells up to 3 mM | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. |
| AID386075 | Drug uptake in human hepatocyte at 2 uM after 16 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386065 | Antiviral activity against HCV 1b Con1 in 2209-23 cells after 72 hrs by luciferase based replicon assay | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID431253 | Antiviral activity against wild type HCV infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay in presence of 100 uM DCTD inhibitor zedularine | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID386300 | Drug uptake in human hepatocyte at 10 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386273 | Drug uptake in human hepatocyte at 2 uM after 16 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrine-2,4(1H,3H)-trione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342058 | Clearance in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341872 | Drug level in rhesus monkey cerebrospinal fluid 2'-deoxy-2'-fluoro-2'-C-methyluridine level at 33.3 mg/kg, po administered as single dose after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID342039 | Metabolic stability in human whole blood at 1000 dpm/pmol after 8 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386280 | Drug uptake in human hepatocyte at 50 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386301 | Drug uptake in human hepatocyte at 25 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341859 | AUC in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341853 | Terminal half life in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341861 | Apparent volume of distribution with respect to bioavailability in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386067 | Inhibition of RNA synthesis activity of HSV 1b Con1 replicase | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386076 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341864 | Mean residence time in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386291 | Drug uptake in human hepatocyte at 100 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341870 | Drug level in rhesus monkey cerebrospinal fluid at 33.3 mg/kg, po administered as single dose after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386071 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386299 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID341876 | Metabolic stability in human whole blood at 1000 dpm/pmol after 0.25 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386069 | Drug uptake in human hepatocyte at 2 uM after 6 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID1071252 | Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
| Nucleotide prodrugs of 2'-deoxy-2'-spirooxetane ribonucleosides as novel inhibitors of the HCV NS5B polymerase. |
| AID278933 | Ratio of Kcat to Km for human dCK expressed in HepG2 cells | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. |
| AID341874 | Oral bioavailability in rhesus monkey at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID1070867 | Inhibition of HCV genotype 1b wild type recombinant NS5B RNA dependent RNA polymerase using IRES RNA as substrate after 30 mins by radioactive assay in presence of [alpha32p]UTP | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5
| Use of 2'-spirocyclic ethers in HCV nucleoside design. |
| AID536905 | Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase. |
| AID386284 | Drug uptake in human hepatocyte at 50 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342059 | Drug level in rhesus monkey serum at 33.3 mg/kg, po administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID1691957 | Antiviral activity against human Norovirus | 2020 | European journal of medicinal chemistry, Jun-01, Volume: 195 | Anti-norovirus activity of C7-modified 4-amino-pyrrolo[2,1-f][1,2,4]triazine C-nucleosides. |
| AID386277 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID493453 | Ratio of Kcat/Km for human recombinant deoxycytidine kinase | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and anti-HCV activity of 3',4'-oxetane nucleosides. |
| AID386077 | Drug uptake in human hepatocyte at 2 uM after 48 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386074 | Drug uptake in human hepatocyte at 2 uM after 6 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID431254 | Antiviral activity against HCV harboring NS5B polymerase S282T mutation infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay in presence of 100 uM DCTD inhibitor zedularine | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
| The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. |
| AID341871 | Drug level in rhesus monkey cerebrospinal fluid assessed as 2'-deoxy-2'-fluoro-2'-C-methyluridine level at 33.3 mg/kg, iv administered as single dose after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386288 | Drug uptake in human hepatocyte at 10 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342060 | Stability in rhesus monkey urine at 33.3 mg/kg assessed as unchanged drug dose administered as single dose during 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID278936 | Activity of human UCK1 expressed in Huh7 cells assessed as phosphorylation by coupled enzyme assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. |
| AID386295 | Drug uptake in human hepatocyte at 25 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342047 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 0.5 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID342053 | Metabolic stability in rhesus monkey whole blood at 1000 dpm/pmol after 24 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386283 | Drug uptake in human hepatocyte at 25 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342036 | Metabolic stability in human whole blood at 1000 dpm/pmol after 1 hr at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID386276 | Drug uptake in human hepatocyte at 2 uM after 72 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimitrine-2,4(1H,3H)-trione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID342041 | Metabolic stability in human whole blood at 1000 dpm/pmol after 24 hrs at 37 degC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID536906 | Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase. |
| AID386281 | Drug uptake in human hepatocyte at 2 uM after 24 hrs assessed as 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one di phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386278 | Drug uptake in human hepatocyte at 10 uM after 24 hrs assessed per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID386303 | Drug uptake in human hepatocyte at 100 uM after 24 hrs assessed as 1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione tri phosphate level per 10'6 cells | 2007 | The Journal of biological chemistry, Oct-12, Volume: 282, Issue:41
| Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. |
| AID246792 | Effective concentration required to reduce cytopathic effects caused by bovine viral diarrhea virus (BVDV) in MDBK cells by 90% | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Design, synthesis, and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methylcytidine, a potent inhibitor of hepatitis C virus replication. |
| AID341858 | AUC in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID342061 | Stability in rhesus monkey urine at 33.3 mg/kg assessed as 2'-deoxy-2'-fluoro-2'-C-methyluridine level administered as single dose during 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID341866 | Volume of distribution at steady state in rhesus monkey at 33.3 mg/kg, iv administered as single dose | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Pharmacokinetics of the antiviral agent beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine in rhesus monkeys. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |