BILN 2061: a macrocyclic NS3 protease inhibitor and antiviral agent; structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 9853710 |
| CHEMBL ID | 297884 |
| SCHEMBL ID | 2524642 |
| MeSH ID | M0457324 |
| Synonym |
|---|
| HY-10242 |
| (cyclopentoxycarbonylamino)-[[2-[2-(isopropylamino)thiazol-4-yl]-7-methoxy-4-quinolyl]oxy]-dioxo-[?]carboxylic acid |
| biln-2061 |
| biln 2061 |
| ciluprevir |
| biln2061 |
| cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5h)-carboxylic acid, 6-[[(cyclopentyloxy)carbonyl]amino]-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydro-2-[[7-methoxy-2-[2-[(1-methylethyl)amino]-4-thiazolyl]-4-quinolinyl]oxy]-5,16-dioxo-, (2 |
| 300832-84-2 |
| (2r,6s,13as,14ar,16as,z)-6-(cyclopentyloxycarbonylamino)-2-(2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yloxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a-carboxyl |
| (1s,4r,6s,14s,18r)-14-cyclopentyloxycarbonylamino-18-[2-(2-isopropylamino-thiazol-4-yl)-7-methoxy-quinolin-4-yloxy]-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.0*4,6*]nonadec-7-ene-4-carboxylic acid |
| (1s,4r,6s,14s,18r)-14-cyclopentyloxycarbonylamino-18-[2-(2-isopropylamino-thiazol-4-yl)-7-methoxy-quinolin-4-yloxy]-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.4,6]nonadec-7-ene-4-carboxylic acid |
| bdbm50142916 |
| (z)-(1s,4r,6s,14s,18r)-14-cyclopentyloxycarbonylamino-18-[2-(2-isopropylamino-thiazol-4-yl)-7-methoxy-quinolin-4-yloxy]-2,15-dioxo-3,16-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid |
| biln 2061 zw |
| CHEMBL297884 , |
| biln-2061-zw |
| ciluprevir [usan:inn] |
| unii-75c8du40t0 |
| 75c8du40t0 , |
| cyclopropa(e)pyrrolo(1,2-a)(1,4)diazacyclopentadecine-14a(5h)-carboxylic acid, 6-(((cyclopentyloxy)carbonyl)amino)-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydro-2-((7-methoxy-2-(2-((1-methylethyl)amino)-4-thiazolyl)-4-quinolinyl)oxy)-5,16-dioxo-, (2 |
| (2r,6s,12z,13as,14ar,16as)-6-(((cyclopentyloxy)carbonyl)amino)-2-((7-methoxy-2-(2-((1-methylethyl)amino)thiazol-4-yl)quinolin-4-yl)oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa(e)pyrrolo(1,2-a)(1,4)diazacyclopentadecine-14a |
| CS-0339 |
| ciluprevir [usan] |
| ciluprevir [inn] |
| (2r,6s,12z,13as,14ar,16as)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[[7-methoxy-2-[2-[(1-methylethyl)amino]thiazol-4-yl]quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a |
| DB05868 |
| F2145-0237 |
| SCHEMBL2524642 |
| AKOS024627485 |
| ciluprevir;biln 2061zw |
| (1s,4r,6s,7z,14s,18r)-14-(cyclopentyloxycarbonylamino)-18-[7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy-2,15-dioxo-3,16-diazatricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid |
| Q5120036 |
| (2r,6s,13as,14ar,16as,z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5h)-car |
| DTXSID50870316 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Genome polyprotein | IC50 | 0.0008 | AID1161415 | |
| Genome polyprotein | Ki | 0.0003 | AID1173945 | |
| Genome polyprotein | IC50 | 3.0000 | AID241120 | |
| Genome polyprotein | Ki | 0.0068 | AID1383023; AID1383024; AID292989 | |
| NS3 protease | Ki | 0.2000 | AID1073073 | |
| Non-structural protein 4A | IC50 | 0.0008 | AID1161415 | |
| Non-structural protein 4A | Ki | 0.0003 | AID1173945 | |
| Cytochrome P450 1A2 | Homo sapiens (human) | Ki | 0.1200 | AID1073074 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.0240 | AID1073072 |
| Cytochrome P450 2D6 | Homo sapiens (human) | Ki | 0.1200 | AID1073074 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Ki | 0.2000 | AID1073073 |
| Cytochrome P450 2C19 | Homo sapiens (human) | Ki | 0.0240 | AID1073072 |
| NS3 protease | Hepatitis C virus subtype 1b | Ki | 0.0720 | AID1073072; AID1073074 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID577352 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577608 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80H mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID322947 | Antiviral activity against Hepatitis C virus infected human hepatoma cells by replicon assay | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 ISSN: 1464-3391 | Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety. |
| AID577377 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577349 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID508189 | Inhibition of Hepatitis C virus genotype 1b NS3/4A protease activity | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID577633 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 V170T mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1242954 | Cytotoxicity against human GS4.1 cells assessed as induction of cell death | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 ISSN: 1464-3405 | Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease. |
| AID577622 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 A156T mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID664167 | Antiviral activity against Hepatitis C virus subtype 1b harboring protease R155K mutant by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID521269 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 V36M/R155K double mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID555950 | Antiviral activity against compound-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID1071917 | Inhibition of Hepatitis C virus genotype 1b NS3 protease domain assessed as equilibrium dissociation constant by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID577357 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R109K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577620 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 A156S mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577625 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168N mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423483 | Drug resistance, ratio of EC50 for HCV 1a H77 with NS5B polymerase G554D mutation to EC50 for wild type HCV 1a H77 infected in chimpanzee measured on day 5 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID423477 | Drug resistance, ratio of EC50 for HCV 1b strain N with NS5B polymerase C316Y mutation to EC50 for wild type HCV 1b strain N infected in chimpanzee measured on day 28 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID1071913 | Inhibition of Hepatitis C virus genotype 1b full-length NS3 protease assessed as overall/observed affinity by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID344556 | Inhibition of full length HCV NS3/4A protease | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 ISSN: 1464-3405 | Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors. |
| AID11485 | Vss was determined | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID573110 | Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH6 cells assessed as reduction in replicon RNA after 4days by RT-qPCR analysis | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID1161416 | Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as inhibition of NS4A expression by ELISA | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 ISSN: 1464-3405 | Structure-based design of a novel series of azetidine inhibitors of the hepatitis C virus NS3/4A serine protease. |
| AID521275 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 T54A mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID577363 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577617 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R155T mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577607 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80R mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID508185 | Antiviral activity against Hepatitis C virus genotype 1b infected in mouse HB1 cell by cell-based HCV replicon assay in presence of 50% normal human serum | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID423480 | Antiviral activity against HCV 1a H77 with NS5B polymerase G554D mutation infected in chimpanzee measured on day 16 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577390 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q41R mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577378 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V170T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID394182 | Antiviral activity against HCV genotype 1 infected in human assessed as reduction in viral titer after 48 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 ISSN: 1520-4804 | Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines. |
| AID1071911 | Inhibition of Hepatitis C virus genotype 1b NS3 protease domain assessed as overall/observed affinity by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID577388 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 V36 M mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID491861 | Antiviral activity against HCV 1B infected in human Huh7 cells by firefly luciferase reporter gene assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 ISSN: 1464-3391 | Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents. |
| AID577614 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R155M mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577364 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1071915 | Inhibition of Hepatitis C virus genotype 1a full-length NS3 protease assessed as overall/observed affinity by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID711483 | Protein binding in human plasma | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID577342 | Antiviral activity against Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1161415 | Inhibition of full length Hepatitis C virus genotype 1b Con1 NS3/4A by FRET assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 ISSN: 1464-3405 | Structure-based design of a novel series of azetidine inhibitors of the hepatitis C virus NS3/4A serine protease. |
| AID612410 | Inhibition of HCV NS3 protease | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 ISSN: 1464-3391 | P2-P1' macrocyclization of P2 phenylglycine based HCV NS3 protease inhibitors using ring-closing metathesis. |
| AID1383026 | Cytotoxicity against human HuH7 cell | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148ISSN: 1768-3254 | Pan-NS3 protease inhibitors of hepatitis C virus based on an R |
| AID1072931 | Inhibition of Hepatitis C virus genotype 1a full length NS3/2K-NS4A protease using Ac-DED(Edans)EEAbupsi[COO]ASK(Dabcyl)-NH2 as substrate incubated for 10 mins prior to substrate addition by FRET analysis | 2014 | ACS medicinal chemistry letters, Mar-13, Volume: 5, Issue:3 ISSN: 1948-5875 | Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region. |
| AID577344 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423474 | Drug resistance, ratio of EC50 for HCV 1b strain N with NS5B polymerase C316Y mutation to EC50 for wild type HCV 1b strain N infected in chimpanzee measured on day 2 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577631 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168V mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423482 | Drug resistance, ratio of EC50 for HCV 1a H77 with NS5B polymerase G554D mutation to EC50 for wild type HCV 1a H77 infected in chimpanzee measured on day 2 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID1383024 | Inhibition of HCV genotype-1a NS3 protease | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148ISSN: 1768-3254 | Pan-NS3 protease inhibitors of hepatitis C virus based on an R |
| AID1383025 | Antiviral activity against HCV genotype 1b infected in human HuH7 cells | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148ISSN: 1768-3254 | Pan-NS3 protease inhibitors of hepatitis C virus based on an R |
| AID328998 | Inhibition of HCV NS3-4A protease | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 ISSN: 1464-3405 | Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor. |
| AID577373 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168Y mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577641 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80R and D168A mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577376 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577371 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423475 | Drug resistance, ratio of EC50 for HCV 1b strain N with NS5B polymerase C316Y mutation to EC50 for wild type HCV 1b strain N infected in chimpanzee measured on day 5 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID521259 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 V170A mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 10 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID1071921 | Inhibition of Hepatitis C virus genotype 1a full-length NS3 protease assessed as equilibrium dissociation constant by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID654781 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh cells by luciferase reporter gene based replicon assay | 2012 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7 ISSN: 1464-3405 | Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease. |
| AID1073074 | Inhibition of full-length HCV NS3 protease A156T mutant | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket. |
| AID146238 | Inhibition of hepatitis C virus in a cell based HCV replicon assay. | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID711485 | Half life in monkey | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID344557 | Inhibition of HCV replication in human HuH7-Rep cells containing subgenomic bicistronic clone | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 ISSN: 1464-3405 | Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors. |
| AID241120 | Inhibitory concentration against hepatitis C virus NS3 protease | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 ISSN: 0022-2623 | Control of hepatitis C: a medicinal chemistry perspective. |
| AID577384 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID711489 | Oral bioavailability in dog | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID577626 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168E mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423469 | Antiviral activity against wild type HCV 1b strain N infected in chimpanzee | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577605 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 T54A mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577628 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168Y mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID521267 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 A156V mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID577380 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S and Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1073075 | Inhibition of full-length wild-type HCV NS3 protease | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket. |
| AID423473 | Antiviral activity against HCV 1b strain N with NS5B polymerase C316Y mutation infected in chimpanzee measured on day 28 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577369 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID555951 | Antiviral activity against cyclosporine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID711491 | Oral bioavailability in rat | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID444180 | Cytotoxicity against human Huh7.5 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 ISSN: 1464-3405 | New small molecule inhibitors of hepatitis C virus. |
| AID555954 | Antiviral activity against BILN 2061-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID521271 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 R155K mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID546789 | Antiviral activity against Hepatitis C virus genotype 1b in luciferase encoding genotype 1b replicons after 3 days by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 ISSN: 1098-6596 | Novel hepatitis C virus reporter replicon cell lines enable efficient antiviral screening against genotype 1a. |
| AID577640 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80H and D168E mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577391 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 F43S mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID711487 | Half life in dog | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID1071918 | Inhibition of Hepatitis C virus genotype 1b full-length NS3/NS4A protease assessed as equilibrium dissociation constant by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID577612 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R109K mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID641102 | Inhibition of Hepatitic C virus NS3/4A protease by FRET assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 ISSN: 1464-3405 | Inhibitory effects of polyphenols toward HCV from the mangrove plant Excoecaria agallocha L. |
| AID173105 | Maximum plasma concentration in rats after oral administration at 20 mg/kg | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID577637 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80K and R155K mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577351 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577623 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 A156V mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID664161 | Antiviral activity against Hepatitis C virus subtype 1b harboring protease D168V mutant by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID322946 | Inhibition of HCV NS3 protease by FRET assay | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 ISSN: 1464-3391 | Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety. |
| AID711502 | Inhibition of HCV 1b NS3 protease | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID577345 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577375 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID521265 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 D168A mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID577362 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577353 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1242952 | Inhibition of full length HCV 1b Con1 NS3/4A protease using HiLyte Fluor 610 peptide substrate by biochemical FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 ISSN: 1464-3405 | Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease. |
| AID664162 | Antiviral activity against Hepatitis C virus subtype 1b harboring protease D168A mutant by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID598530 | Antiviral activity against HCV genotype 1b infected in Huh7 cells assessed as inhibition of viral replication by cell-based replicon assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 ISSN: 1464-3405 | Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease. |
| AID577387 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 V36L mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID664163 | Antiviral activity against Hepatitis C virus subtype 1b harboring protease A156V mutant by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID423471 | Antiviral activity against HCV 1b strain N with NS5B polymerase C316Y mutation infected in chimpanzee measured on day 5 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID423481 | Antiviral activity against HCV 1a H77 with NS5B polymerase Y448C mutation infected in chimpanzee measured on day 28 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577354 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577361 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155Q mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577606 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 T54S mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577386 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423470 | Antiviral activity against HCV 1b strain N with NS5B polymerase C316Y mutation infected in chimpanzee measured on day 2 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID423484 | Drug resistance, ratio of EC50 for HCV 1a H77 with NS5B polymerase G554D mutation to EC50 for wild type HCV 1a H77 infected in chimpanzee measured on day 16 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID12746 | Area under the plasma concentration-time curve in rats after oral administration at 20 mg/kg | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID577635 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 F43S and Q80R mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID146239 | Inhibitory concentration against hepatitis C virus NS3 protease | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID523615 | Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Mechanism of resistance of hepatitis C virus replicons to structurally distinct cyclophilin inhibitors. |
| AID577613 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 S138T mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577383 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID521266 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 D168V mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID444179 | Antiviral activity against HCV2a J6/JFH1 infected in Huh7-5 cells assessed as inhibition of core protein dimerization by RT PCR | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 ISSN: 1464-3405 | New small molecule inhibitors of hepatitis C virus. |
| AID577367 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID595272 | Antiviral activity against Hepatitis C virus infected in human Ava5 cells assessed as decreased NS3 protein level at 20 nM after 72 hrs by Western blotting | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 ISSN: 1520-6025 | Diosgenin, a plant-derived sapogenin, exhibits antiviral activity in vitro against hepatitis C virus. |
| AID664159 | Antiviral activity against Hepatitis C virus subtype 1b by stable replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID521273 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 V36M mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID444181 | Antiviral activity against HCV2a J6/JFH1 infected in Huh7-5 cells at early T1 stage assessed as inhibition of core protein dimerization by RT PCR | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 ISSN: 1464-3405 | New small molecule inhibitors of hepatitis C virus. |
| AID577632 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168I mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577347 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID521255 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 D168V mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 100 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID509556 | Inhibition of HCV NS3 protease | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 ISSN: 1520-4804 | Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335). |
| AID180765 | Bioavailability in rat (dose 5 mg/kg i.v.) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID598531 | Inhibition of HCV 1a NS3/4A protease | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 ISSN: 1464-3405 | Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease. |
| AID509557 | Antiviral activity against HCV Con1 by cell based-luciferase reporter gene assay | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 ISSN: 1520-4804 | Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335). |
| AID577603 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 F43I mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577381 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID491860 | Inhibition of HCV NS3 protease by FRET assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 ISSN: 1464-3391 | Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents. |
| AID508188 | Inhibition of Hepatitis C virus genotype 2a NS3/4A protease activity | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID577358 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 S138T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID555952 | Antiviral activity against 2'-C-methyl-2'-fluoro-cytidine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID664165 | Antiviral activity against Hepatitis C virus subtype 1b harboring protease A156S mutant by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID573108 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID394178 | Antiviral activity against HCV isolate Con1 in human Huh7 cells assessed as reduction in viral RNA after 7 days by RT-PCR | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 ISSN: 1520-4804 | Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines. |
| AID577611 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80L mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423478 | Antiviral activity against HCV 1a H77 with NS5B polymerase G554D mutation infected in chimpanzee measured on day 2 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577629 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168H mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID649649 | Antiviral activity against HCV genotype 1b infected in human Huh cells expressing luc gene by replicon assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 ISSN: 1464-3405 | Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity. |
| AID171332 | Plasma clearance after intravenous administration at 5 mg/kg in rats | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID423476 | Drug resistance, ratio of EC50 for HCV 1b strain N with NS5B polymerase C316Y mutation to EC50 for wild type HCV 1b strain N infected in chimpanzee measured on day 11 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID612408 | Antiviral activity against HCV | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 ISSN: 1464-3391 | P2-P1' macrocyclization of P2 phenylglycine based HCV NS3 protease inhibitors using ring-closing metathesis. |
| AID573106 | Cytotoxicity against human Huh-9-13 cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID444182 | Antiviral activity against HCV2a J6/JFH1 infected in Huh7-5 cells at late T2 stage assessed as inhibition of core protein dimerization by RT PCR | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 ISSN: 1464-3405 | New small molecule inhibitors of hepatitis C virus. |
| AID577348 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID508186 | Antiviral activity against Hepatitis C virus genotype 1b infected in mouse HB1 cell by cell-based HCV replicon assay in presence of 10% fetal bovine serum | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID577382 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577616 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R155Q mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577389 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 V36A mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID546790 | Antiviral activity against Hepatitis C virus genotype 1a in luciferase encoding genotype 1a replicons after 3 days by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 ISSN: 1098-6596 | Novel hepatitis C virus reporter replicon cell lines enable efficient antiviral screening against genotype 1a. |
| AID577634 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 V170A mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577610 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80G mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID711486 | Half life in rat | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID322793 | Inhibition of RNA copy numbers in HCV 1b-N replicon cells with NS5B M414T mutant at EC50 after 4 days | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 ISSN: 0066-4804 | Evolution of resistant M414T mutants among hepatitis C virus replicon cells treated with polymerase inhibitor A-782759. |
| AID711501 | Inhibition of HCV 1a NS3 protease | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID573105 | Cytotoxicity against human HuH6 cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID664160 | Antiviral activity against Hepatitis C virus subtype 1a by stable replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID577618 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R155K mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577385 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80H and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577615 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R155I mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID521256 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 A156T mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 100 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID577355 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1071920 | Inhibition of Hepatitis C virus genotype 1a full-length NS3/NS4A protease assessed as equilibrium dissociation constant by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID521268 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 A156S mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID1645924 | Antiviral activity against HCV | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164ISSN: 1768-3254 | A review on HCV inhibitors: Significance of non-structural polyproteins. |
| AID322795 | Inhibition of RNA copy numbers in HCV 1b-N replicon cells with NS5B M414T mutant at 100 times EC50 after 4 days | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 ISSN: 0066-4804 | Evolution of resistant M414T mutants among hepatitis C virus replicon cells treated with polymerase inhibitor A-782759. |
| AID577350 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577374 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577639 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80R and D168E mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID555943 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 5 passages at 1 uM by quantitative RT-PCR relative to wild type virus | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID577356 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID573107 | Cytotoxicity against human Huh-Mono cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID591091 | Cytotoxicity against human Huh7.5 cells | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3405 | Potent inhibitors of hepatitis C core dimerization as new leads for anti-hepatitis C agents. |
| AID521270 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 A156T mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID521263 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 R155K mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 10 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID292989 | Inhibition of HCV 1a NS3 protease | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 ISSN: 0968-0896 | Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors. |
| AID711490 | Antiviral activity against HCV1b by cell based replicon assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID1072927 | Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells by subgenomic replicon-based luciferase assay | 2014 | ACS medicinal chemistry letters, Mar-13, Volume: 5, Issue:3 ISSN: 1948-5875 | Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region. |
| AID1173954 | Antiviral activity against HCV genotype 1a | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 ISSN: 1464-3391 | Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles. |
| AID508187 | Inhibition of Hepatitis C virus genotype 2b NS3/4A protease activity | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID577604 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 F43V mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID328999 | Antiviral activity against HCV replicon | 2008 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8 ISSN: 1464-3405 | Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor. |
| AID508190 | Inhibition of Hepatitis C virus genotype 1a NS3/4A protease activity | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID394177 | Antiviral activity against HCV 1a containing chimeric genotype 1a-H77/1b-con1 subgenom in human Huh7 cells assessed as reduction in viral RNA after 7 days by RT-PCR | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 ISSN: 1520-4804 | Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines. |
| AID322796 | Antiviral activity against HCV 1b-N | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 ISSN: 0066-4804 | Evolution of resistant M414T mutants among hepatitis C virus replicon cells treated with polymerase inhibitor A-782759. |
| AID423485 | Drug resistance, ratio of EC50 for HCV 1a H77 with NS5B polymerase Y448C mutation to EC50 for wild type HCV 1a H77 infected in chimpanzee measured on day 28 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID577638 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80R and R155K mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1383023 | Inhibition of HCV genotype-3a full length NS3 protease preincubated for 10 mins followed by Ac-DED(Edans)EEAbuj-[COO]ASK(Dabcyl)-NH2 addition in presence of co-factor 2K-NS4A by fluorescence assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148ISSN: 1768-3254 | Pan-NS3 protease inhibitors of hepatitis C virus based on an R |
| AID521274 | Antiviral activity against wild-type Hepatitis C virus genotype 1b N infected in human Huh7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID521272 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 R155Q mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID654780 | Inhibition of Hepatitis C virus genotype 1b NS3/4A protease | 2012 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7 ISSN: 1464-3405 | Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease. |
| AID577609 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 Q80K mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID664158 | Inhibition of HCV 1a protease 1a domain | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID577366 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577343 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1173945 | Inhibition of HCV genotype 1a NS3/4A protease using Ac-DED(Edans)EEAbu-psi[COO]ASK(Dabcyl)-NH2 as substrate by FRET assay | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23 ISSN: 1464-3391 | Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles. |
| AID591089 | Antiviral activity against Hepatitis C virus JFH-1 J6 infected in human HuH7.5 cells assessed as inhibition of virus propagation measured after 72 hrs | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3405 | Potent inhibitors of hepatitis C core dimerization as new leads for anti-hepatitis C agents. |
| AID1071914 | Inhibition of Hepatitis C virus genotype 1a full-length NS3/NS4A protease assessed as overall/observed affinity by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID573111 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-Mono cells assessed as reduction in replicon RNA after 4 days by RT-qPCR analysis | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID664166 | Antiviral activity against wild type Hepatitis C virus subtype 1b by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID1071910 | Inhibition of Hepatitis C virus genotype 3a full-length NS3 protease assessed as overall/observed affinity by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID521261 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 A156T mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 10 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID577368 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1071916 | Inhibition of Hepatitis C virus genotype 3a full-length NS3 protease assessed as equilibrium dissociation constant by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID711488 | Oral bioavailability in monkey | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID10630 | Half-life period in rats after intravenous administration at 5 mg/kg | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 ISSN: 0022-2623 | Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. |
| AID555953 | Antiviral activity against R479-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID711492 | Antiviral activity against HCV1a by cell based replicon assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 ISSN: 1520-4804 | Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
| AID577379 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V170A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID573112 | Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID555941 | Antiviral activity against HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication selected after 5 passages at 1 uM by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID577636 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 F43S and D168E mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1073072 | Inhibition of full-length HCV NS3 protease R155K mutant | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket. |
| AID1071919 | Inhibition of Hepatitis C virus genotype 1b full-length NS3 protease assessed as equilibrium dissociation constant by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID423479 | Antiviral activity against HCV 1a H77 with NS5B polymerase G554D mutation infected in chimpanzee measured on day 5 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID521258 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 R155K mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 100 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID292988 | Inhibition of HCV 1b NS3 protease | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3 ISSN: 0968-0896 | Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors. |
| AID577359 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577372 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID521264 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 V170A mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID521276 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 V170A mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 100 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID508184 | Antiviral activity against Hepatitis C virus genotype 2a infected in mouse HB1 cell by cell-based HCV replicon assay in presence of 10% fetal bovine serum | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID577621 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 A156G mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID344558 | Metabolic stability in human liver microsomess after 15 mins at 5 uM | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 ISSN: 1464-3405 | Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors. |
| AID577365 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID664164 | Antiviral activity against Hepatitis C virus subtype 1b harboring protease A156T mutant by transient replicon assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 ISSN: 1520-4804 | Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants. |
| AID1242953 | Antiviral activity against HCV Con1 infected in human GS4.1 cells containing HCV Con1 subgenomic replicon assessed as reduction in NS5A protein expression by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 ISSN: 1464-3405 | Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease. |
| AID577627 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168T mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID591090 | Antiviral activity against Hepatitis C virus JFH-1 J6 infected in human HuH7.5 cells assessed as inhibition of virus propagation measured after 72 hrs of transfer to fresh media | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 ISSN: 1464-3405 | Potent inhibitors of hepatitis C core dimerization as new leads for anti-hepatitis C agents. |
| AID555955 | Antiviral activity against VX 950-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 ISSN: 1098-6596 | Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. |
| AID322794 | Inhibition of RNA copy numbers in HCV 1b-N replicon cells with NS5B M414T mutant at 10 times EC50 after 4 days | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 ISSN: 0066-4804 | Evolution of resistant M414T mutants among hepatitis C virus replicon cells treated with polymerase inhibitor A-782759. |
| AID577630 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168A mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577619 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 R155G mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID649647 | Inhibition of HCV1b NS3/4A protease | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 ISSN: 1464-3405 | Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity. |
| AID521257 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 R155Q mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 100 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID1071912 | Inhibition of Hepatitis C virus genotype 1b full-length NS3/NS4A protease assessed as overall/observed affinity by surface plasmon resonance biosensor-based interaction kinetic analysis | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. |
| AID523614 | Antiviral activity against cyclosporine A/NIM811-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Mechanism of resistance of hepatitis C virus replicons to structurally distinct cyclophilin inhibitors. |
| AID577360 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID573109 | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-9-13 cells assessed as reduction in replicon RNA after 4days by RT-qPCR analysis | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 ISSN: 1098-6596 | Comparative in vitro anti-hepatitis C virus activities of a selected series of polymerase, protease, and helicase inhibitors. |
| AID521262 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 R155Q mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 10 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID577370 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168N mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID423472 | Antiviral activity against HCV 1b strain N with NS5B polymerase C316Y mutation infected in chimpanzee measured on day 11 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 ISSN: 0066-4804 | Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. |
| AID508183 | Cytotoxicity against mouse HB-1 cells | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1 ISSN: 1098-6596 | MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
| AID577346 | Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q41R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID577624 | Ratio of EC50 for Hepatitis C virus subtype 1b expressing NS3 D168G mutant to EC50 for Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. |
| AID1073073 | Inhibition of full-length HCV NS3 protease D168V mutant | 2014 | Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5 ISSN: 1520-4804 | Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket. |
| AID521260 | Selectivity ratio of EC50 for Hepatitis C virus genotype 1b N expressing NS3 D168V mutant infected in human HuH7 cells to EC50 for Hepatitis C virus genotype 1b N expressing wild type NS3 infected in human HuH7 cells at 10 nM | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 ISSN: 0066-4804 | Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system. |
| AID1799853 | Competitive Inhibition Assay from Article 10.1021/bi9016928: \\Hepatitis C virus NS3 protease is activated by low concentrations of protease inhibitors.\\ | 2009 | Biochemistry, Dec-08, Volume: 48, Issue:48 ISSN: 1520-4995 | Hepatitis C virus NS3 protease is activated by low concentrations of protease inhibitors. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 47 (56.63) | 29.6817 |
| 2010's | 36 (43.37) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 7 (8.33%) | 5.53% |
| Reviews | 3 (3.57%) | 6.00% |
| Case Studies | 1 (1.19%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 73 (86.90%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cardiac Diseases | 0 | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Chronic Hepatitis C | 0 | 2004 | 2015 | 16.6 | medium | 5 | 0 | 0 | 6 | 2 | 0 | |
| Disease Models, Animal | 0 | 2006 | 2007 | 17.7 | low | 0 | 0 | 0 | 3 | 0 | 0 | |
| Heart Diseases | 0 | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Hepatitis C | 0 | 2003 | 2019 | 16.0 | high | 2 | 0 | 0 | 17 | 5 | 0 | |
| Hepatitis C, Chronic | 0 | 2004 | 2015 | 16.6 | medium | 5 | 0 | 0 | 6 | 2 | 0 | |
| Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted | 0 | 2003 | 2019 | 16.0 | high | 2 | 0 | 0 | 17 | 5 | 0 | |
| Sensitivity and Specificity | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Article | Year |
|---|---|
| Ultra-rapid cardiotoxicity of the hepatitis C virus protease inhibitor BILN 2061 in the urokinase-type plasminogen activator mouse. Gastroenterology, , Volume: 133, Issue:4 | 2007 |
| Article | Year |
|---|---|
| A twenty-eight-day mechanistic time course study in the rhesus monkey with hepatitis C virus protease inhibitor BILN 2061. Toxicologic pathology, , Volume: 39, Issue:3 | 2011 |
| Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines. Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6 | 2009 |
| Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. Antimicrobial agents and chemotherapy, , Volume: 51, Issue:12 | 2007 |
| Article | Year |
|---|---|
| Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. Antimicrobial agents and chemotherapy, , Volume: 53, Issue:3 | 2009 |