Page last updated: 2024-12-11
biln 2061
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Research Excerpts
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Description
BILN 2061: a macrocyclic NS3 protease inhibitor and antiviral agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9853710 |
| CHEMBL ID | 297884 |
| SCHEMBL ID | 2524642 |
| MeSH ID | M0457324 |
Synonyms (34)
| 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 |
Research Excerpts
Overview
BILN 2061 is a novel, specific hepatitis C virus (HCV) NS3 serine protease inhibitor discovered by Boehringer Ingelheim. It has shown potent activity against HCV replicons in tissue culture and is under clinical investigation for the treatment of HCV infection.
Compound-Compound Interactions
| Excerpt | Reference | Relevance |
|---|---|---|
| "6 log(10) units was obtained in phase II studies when Debio 025 was combined with interferon (R." | ( 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. Coelmont, L; Dumont, JM; Kaptein, S; Neyts, J; Paeshuyse, J; Vliegen, I; Vuagniaux, G, 2009) | 0.35 |
Bioavailability
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " The design included oral dosing of 30 mg per kg of body weight twice a day for 14 days, followed by a 14-day posttreatment observation." | ( Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model. Beno, DW; Bosse, TD; Chen, CM; He, Y; Hernandez, LE; Kati, WM; Kempf, DJ; Kohlbrenner, WE; Lanford, RE; Larson, DP; Lim, HB; Long, MA; Lu, L; Middleton, T; Molla, A; Pilot-Matias, TJ; Tripathi, RL; Wagner, R, 2007) | 0.34 |
| " Echocardiographic traces obtained after twenty-eight consecutive days of dosing revealed two animals with diminished left ventricular cardiac ejection fraction." | ( A twenty-eight-day mechanistic time course study in the rhesus monkey with hepatitis C virus protease inhibitor BILN 2061. Huang, Q; Knight, BL; Pack, FD; Seidler, RW; Stern, JO; Stoltz, JH, 2011) | 0.58 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (10)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Genome polyprotein | IC50 (µMol) | 0.0008 | 0.0000 | 0.0289 | 0.1870 | AID1161415 | |
| Genome polyprotein | Ki | 0.0003 | 0.0000 | 0.0067 | 0.0300 | AID1173945 | |
| Genome polyprotein | IC50 (µMol) | 3.0000 | 0.7000 | 1.9567 | 3.8000 | AID241120 | |
| Genome polyprotein | Ki | 0.0068 | 0.0000 | 0.0028 | 0.0200 | AID1383023; AID1383024; AID292989 | |
| NS3 protease | Ki | 0.2000 | 0.0039 | 0.0829 | 0.2000 | AID1073073 | |
| Non-structural protein 4A | IC50 (µMol) | 0.0008 | 0.0000 | 0.0289 | 0.1870 | AID1161415 | |
| Non-structural protein 4A | Ki | 0.0003 | 0.0000 | 0.0067 | 0.0300 | AID1173945 | |
| Cytochrome P450 1A2 | Homo sapiens (human) | Ki | 0.1200 | 0.0056 | 1.1534 | 9.0000 | AID1073074 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.0240 | 0.0001 | 1.4162 | 9.9000 | AID1073072 |
| Cytochrome P450 2D6 | Homo sapiens (human) | Ki | 0.1200 | 0.0001 | 1.1986 | 8.0000 | AID1073074 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Ki | 0.2000 | 0.0003 | 1.6842 | 10.0000 | AID1073073 |
| Cytochrome P450 2C19 | Homo sapiens (human) | Ki | 0.0240 | 0.0001 | 0.8300 | 10.0000 | AID1073072 |
| NS3 protease | Hepatitis C virus subtype 1b | Ki | 0.0720 | 0.0090 | 1.2670 | 6.1000 | AID1073072; AID1073074 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (42)
Molecular Functions (34)
Ceullar Components (6)
Bioassays (254)
| 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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: 148 | 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 | 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 | 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 | 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 | 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 | 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: 148 | 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: 148 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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: 164 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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: 148 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | Hepatitis C virus NS3 protease is activated by low concentrations of protease inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (83)
| 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 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 17.48
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.48) All Compounds (24.57) |
Study Types
| 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% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||