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show all sequences of 3.4.21.98

Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor

McCauley, J.A.; McIntyre, C.J.; Rudd, M.T.; Nguyen, K.T.; Romano, J.J.; Butcher, J.W.; Gilbert, K.F.; Bush, K.J.; Holloway, M.K.; Swestock, J.; Wan, B.L.; Carroll, S.S.; DiMuzio, J.M.; Graham, D.J.; Ludmerer, S.W.; Mao, S.S.; Stahlhut, M.W.; Fandozzi, C.M.; Trainor, N.; Olsen, D.B.; Vacca, J.P.; Liverton, N.J.; J. Med. Chem. 53, 2443-2463 (2010)

Data extracted from this reference:

Inhibitors
Inhibitors
Commentary
Organism
Structure
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
-
Hepacivirus C
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
-
Hepacivirus C
(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
Hepacivirus C
(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
Hepacivirus C
(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(2R,4S,7S,14Z)-7-tert-butyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-6,9-dioxo-3,4,6,7,8,9,12,13-octahydro-2H,11H-16,18-etheno-2,5-methanopyrido[2,3-k][1,10,3,6]dioxadiazacyclononadecine-4-carboxamide
-
Hepacivirus C
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
-
Hepacivirus C
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
-
Hepacivirus C
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
-
Hepacivirus C
BILN-2061
rapidly reversible NS3 inhibitor
Hepacivirus C
boceprevir
SCH 503034, slowly reversible covalent inhibitor
Hepacivirus C
ITMN-191
rapidly reversible inhibitor
Hepacivirus C
telaprevir
VX-950, slowly reversible covalent inhibitor
Hepacivirus C
TMC 435350
rapidly reversible inhibitor
Hepacivirus C
vaniprevir
; MK-7009, i.e. (1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
Hepacivirus C
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Hepacivirus C
-
genotype 1b
-
Ki Value [mM]
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
0.00000002
-
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000002
-
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
Ki below 0.00000002 mM, in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000003
-
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000004
-
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000004
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000004
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
vaniprevir
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000006
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000008
-
(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000009
-
(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000009
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000009
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000001
-
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000001
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000014
-
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000015
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000018
-
(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000003
-
(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000045
-
(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000122
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000016
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000083
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
Hepacivirus C
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
Hepacivirus C
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
-
Hepacivirus C
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
-
Hepacivirus C
(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
Hepacivirus C
(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
Hepacivirus C
(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
Hepacivirus C
(2R,4S,7S,14Z)-7-tert-butyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-6,9-dioxo-3,4,6,7,8,9,12,13-octahydro-2H,11H-16,18-etheno-2,5-methanopyrido[2,3-k][1,10,3,6]dioxadiazacyclononadecine-4-carboxamide
-
Hepacivirus C
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
-
Hepacivirus C
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
-
Hepacivirus C
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
-
Hepacivirus C
BILN-2061
rapidly reversible NS3 inhibitor
Hepacivirus C
boceprevir
SCH 503034, slowly reversible covalent inhibitor
Hepacivirus C
ITMN-191
rapidly reversible inhibitor
Hepacivirus C
telaprevir
VX-950, slowly reversible covalent inhibitor
Hepacivirus C
TMC 435350
rapidly reversible inhibitor
Hepacivirus C
vaniprevir
; MK-7009, i.e. (1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
Hepacivirus C
Ki Value [mM] (protein specific)
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
0.00000002
-
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000002
-
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
Ki below 0.00000002 mM, in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000003
-
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000004
-
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000004
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000004
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000005
-
vaniprevir
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000006
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000008
-
(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000009
-
(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000009
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000009
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000001
-
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000001
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000014
-
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000015
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000018
-
(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000003
-
(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000045
-
(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.00000122
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000016
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
0.0000083
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
Hepacivirus C
Other publictions for EC 3.4.21.98
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
731457
Parsy
Structure-based design of a no ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
24
4444-4449
2014
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731460
Kirschberg
Novel, sulfonamide linked inhi ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
24
969-972
2014
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731890
Morikawa
Quantitative proteomics identi ...
Hepacivirus C
Hepatology
59
423-433
2014
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732197
Rimmert
A 3D structural model and dyna ...
Hepacivirus C, Hepacivirus C ED43
J. Biomol. Struct. Dyn.
32
950-958
2014
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732226
Meeprasert
Key binding and susceptibility ...
Hepacivirus C
J. Chem. Inf. Model.
54
1208-1217
2014
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732266
Brenndoerfer
Cleavage of the T cell protein ...
Hepacivirus C
J. Immunol.
192
1671-1680
2014
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1
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732311
LaPlante
Ligand bioactive conformation ...
Hepacivirus C
J. Med. Chem.
57
1777-1789
2014
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732489
Lan
Establishment of a novel tripl ...
Hepacivirus C
Mol. Biol. Rep.
41
7349-7359
2014
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1
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731144
Jiang
In vitro phenotypic characteri ...
Hepacivirus C
Antimicrob. Agents Chemother.
57
6236-6245
2013
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34
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731444
Bondada
Azetidines and spiro azetidine ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
23
6325-6330
2013
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732738
Abian
Allosteric inhibitors of the N ...
Hepacivirus C
PLoS ONE
8
e69773
2013
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731743
Ding
Hepatitis C virus NS3/4A prote ...
Hepacivirus C
Eur. J. Immunol.
42
2374-2382
2012
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732702
Parera
Canine hepacivirus NS3 serine ...
canine hepacivirus
PLoS ONE
7
e42481
2012
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717315
Martin
In-cell selectivity profiling ...
Hepacivirus C
Biol. Chem.
392
927-935
2011
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717347
Clarke
Novel, potent, and orally bioa ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
21
3568-3572
2011
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717962
Liu
Screening and rank ordering of ...
Hepacivirus C
J. Mass Spectrom.
46
764-771
2011
1
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718016
Geitmann
Mechanistic and kinetic charac ...
Hepacivirus C
J. Mol. Recognit.
24
60-70
2011
1
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718059
Aparicio
Complexity and catalytic effic ...
Hepacivirus C
J. Virol.
85
5961-5969
2011
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718060
Romano
Molecular mechanisms of viral ...
Hepacivirus C
J. Virol.
85
6106-6116
2011
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707170
Lenz
In vitro resistance profile of ...
Hepacivirus C
Antimicrob. Agents Chemother.
54
1878-1887
2010
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5
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707172
Liverton
MK-7009, a potent and selectiv ...
Hepacivirus C
Antimicrob. Agents Chemother.
54
305-311
2010
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15
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707181
Salloum
The resistance mutation R155K ...
Hepacivirus C
Antiviral Res.
87
272-275
2010
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3
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707182
Wang
Bioluminescence imaging of Hep ...
Hepacivirus C
Antiviral Res.
87
50-56
2010
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707301
Peres-da-Silva
Mutations in hepatitis C virus ...
Hepacivirus C
Arch. Virol.
155
807-811
2010
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6
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707390
Massariol
Protease and helicase activiti ...
Hepacivirus C
Biochem. Biophys. Res. Commun.
391
692-697
2010
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5
709473
McCauley
Discovery of vaniprevir (MK-70 ...
Hepacivirus C
J. Med. Chem.
53
2443-2463
2010
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709748
Lemm
Identification of hepatitis C ...
Hepacivirus C
J. Virol.
84
482-491
2010
1
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717325
Nilsson
Synthesis and SAR of potent in ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
20
4004-4011
2010
-
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18
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4
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18
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18
18
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-
717367
Bogen
Discovery of potent sulfonamid ...
Hepacivirus C
Bioorg. Med. Chem.
18
1854-1865
2010
-
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21
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5
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17
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17
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-
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-
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717388
Abian
Conformational stability of he ...
Hepacivirus C
Biophys. J.
99
3811-3820
2010
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1
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1
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-
695639
Lin
In vitro activity and preclini ...
Hepacivirus C, Hepatitis C virus subtype 1a
Antimicrob. Agents Chemother.
53
1377-1385
2009
-
2
2
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-
-
2
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5
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2
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2
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2
2
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2
2
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-
2
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695940
Dansako
Double-stranded RNA-induced in ...
Hepacivirus C
Arch. Virol.
154
801-810
2009
-
1
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2
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2
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3
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2
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2
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1
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2
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2
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2
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-
2
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696672
Avolio
Inhibitors of hepatitis C viru ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
19
2295-2298
2009
-
-
-
-
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12
-
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2
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12
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12
12
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-
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-
-
-
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-
-
-
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-
-
-
-
697520
Mederacke
Boceprevir, an NS3 serine prot ...
Hepacivirus C
Curr. Opin. Investig. Drugs
10
181-189
2009
-
-
-
-
-
-
1
-
1
-
-
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-
2
-
-
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1
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1
1
-
1
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-
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-
-
-
-
-
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707153
El Hefnawi
Natural genetic engineering of ...
Hepacivirus C
Ann. N. Y. Acad. Sci.
1178
173-185
2009
-
-
-
-
-
-
-
-
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1
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1
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-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707507
Thibeault
Use of the fused NS4A peptide- ...
Hepacivirus C, Hepacivirus C J
Biochemistry
48
744-753
2009
1
-
1
-
1
1
9
2
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-
-
-
-
2
-
-
1
-
-
-
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-
2
-
-
-
-
2
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16
-
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1
-
1
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-
1
1
-
9
16
2
-
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-
-
-
-
-
1
-
-
-
-
2
-
-
-
-
2
-
-
-
-
-
-
-
-
2
2
685533
Chen
Potent and selective small mol ...
Hepacivirus C
Bioorg. Med. Chem.
16
1874-1883
2008
-
1
-
-
-
-
14
-
-
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5
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13
-
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1
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14
13
-
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-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
690462
Zhou
Phenotypic characterization of ...
Hepacivirus C, Hepacivirus C H
Antimicrob. Agents Chemother.
52
110-120
2008
-
-
1
1
12
-
3
6
-
-
-
-
-
5
-
-
1
-
-
-
-
-
4
1
-
-
-
-
-
-
-
2
-
-
6
-
-
1
2
1
12
-
6
3
-
6
-
-
-
-
-
-
-
1
-
-
-
-
4
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
695249
Cubero
Naturally occurring NS3-protea ...
Hepacivirus C
Virology
370
237-245
2008
-
1
-
-
1
-
-
-
-
-
-
-
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3
-
-
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-
-
-
-
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-
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-
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-
-
-
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-
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2
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-
-
2
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-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
695259
Franco
A wide range of NS3/4A proteas ...
Hepacivirus C
Virus Res.
131
260-270
2008
-
1
1
-
-
-
-
-
-
-
-
-
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12
-
-
-
-
-
-
-
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12
-
-
-
-
-
-
-
-
1
-
-
-
-
11
11
11
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
12
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
695646
Helbig
A screening method for identif ...
Hepacivirus C
Antiviral Res.
77
169-176
2008
-
1
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696633
Bogen
Hepatitis C virus NS3-4A serin ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
18
4219-4223
2008
-
-
-
-
-
-
11
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
11
-
-
-
-
-
-
-
-
-
-
11
11
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696640
Raboisson
Discovery of novel potent and ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
18
5095-5100
2008
-
-
-
-
-
-
1
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
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-
-
-
-
-
-
-
-
-
1
1
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-
-
-
-
-
-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697173
Rebsamen
The antiviral adaptor proteins ...
Hepacivirus C
Cell Death Differ.
15
1804-1811
2008
-
-
-
-
-
-
-
-
-
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1
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4
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-
-
-
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-
-
1
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-
-
-
-
-
-
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-
-
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-
-
-
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-
1
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-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
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681172
Loehr
Yellow fever virus NS3 proteas ...
Yellow fever virus
J. Gen. Virol.
88
2223-2227
2007
1
1
1
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1
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16
2
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1
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-
1
-
-
-
-
-
2
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-
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-
2
1
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-
1
15
-
-
1
1
1
1
-
1
-
-
16
15
2
-
-
-
-
-
-
-
1
-
-
-
-
2
-
-
-
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2
1
-
-
-
-
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681415
Tedbury
Characterisation of the role o ...
Hepacivirus C
J. Mol. Biol.
366
1652-1660
2007
1
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1
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10
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3
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1
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1
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-
-
-
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2
-
-
-
-
-
-
-
-
-
-
-
7
1
-
1
-
-
10
-
7
3
-
-
-
1
2
-
-
-
-
1
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
684506
Zuo
Activity of compounds from Chi ...
Hepacivirus C
Antiviral Res.
76
86-92
2007
-
1
1
-
-
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5
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
8
-
1
1
1
-
-
-
8
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
685513
Li
Prediction of binding for a ki ...
Hepacivirus C
Bioorg. Med. Chem.
15
220-226
2007
-
1
-
-
-
-
6
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
5
-
1
-
-
-
-
-
5
6
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
688374
Mastrangelo
Crystal structure and activity ...
Kunjin virus
J. Mol. Biol.
372
444-455
2007
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
690304
De Francesco
Advances in the development of ...
Hepacivirus C
Adv. Drug Deliv. Rev.
59
1242-1262
2007
-
1
-
1
18
-
6
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3
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-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
1
1
-
2
-
1
-
1
1
18
-
2
6
1
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
690400
Konstantinidis
Longer wavelength fluorescence ...
Hepacivirus C
Anal. Biochem.
368
156-167
2007
-
-
1
-
-
-
3
4
-
-
-
-
-
2
-
-
1
-
-
-
-
1
2
-
-
-
-
4
-
-
-
-
5
-
-
-
-
1
-
-
-
-
-
3
5
4
-
-
-
-
-
-
-
1
-
-
-
1
2
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
691208
Baeck
Novel potent macrocyclic inhib ...
Hepacivirus C
Bioorg. Med. Chem.
15
7184-7202
2007
-
-
1
-
-
-
17
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
15
-
-
-
-
1
1
-
-
-
-
17
15
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
691209
Thorstensson
Synthesis of novel potent hepa ...
Hepacivirus C
Bioorg. Med. Chem.
15
827-838
2007
-
1
-
-
-
-
19
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
19
-
-
-
1
-
1
-
-
-
-
19
19
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
691969
Venkatraman
Macrocyclic inhibitors of HCV ...
Hepacivirus C
Curr. Top. Med. Chem.
7
1290-1301
2007
-
-
-
1
-
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69
-
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1
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-
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2
-
-
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-
-
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-
-
-
1
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-
-
-
-
-
1
54
-
14
-
-
-
1
1
-
-
14
69
54
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
692986
Johnson
Functional and therapeutic ana ...
Hepacivirus C
J. Biol. Chem.
282
10792-10803
2007
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1
1
-
2
-
2
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
1
1
1
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
692999
Zhou
Phenotypic and structural anal ...
Hepacivirus C
J. Biol. Chem.
282
22619-22628
2007
-
1
1
1
6
-
3
4
-
-
-
-
-
3
-
-
1
-
-
-
-
1
1
-
-
-
-
-
-
-
-
2
-
-
9
-
1
1
2
1
6
-
9
3
-
4
-
-
-
-
-
-
-
1
-
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
693388
Poliakov
Mechanistic studies of electro ...
Hepacivirus C
J. Enzyme Inhib. Med. Chem.
22
191-199
2007
-
-
-
-
-
-
10
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
36
-
-
-
-
-
1
-
-
-
-
10
36
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
693699
Rosales-Leon
Analysis of the domain interac ...
Dengue virus, Hepacivirus C
J. Mol. Graph. Model.
25
585-594
2007
-
2
-
-
-
-
-
-
-
-
-
-
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5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
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A quantum mechanics/molecular ...
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Cleavage targets and the D-arg ...
West Nile virus
Biochem. J.
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Impact of naturally occurring ...
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Biochemistry
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Novel inhibitors of hepatitis ...
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Bioorg. Med. Chem. Lett.
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11
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Potent 7-hydroxy-1,2,3,4-tetra ...
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3
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Novel potent hepatitis C virus ...
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10
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10
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681224
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A complete mutational fitness ...
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691207
Johansson
Potent inhibitors of the hepat ...
Hepacivirus C
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691253
Arasappan
P2-P4 macrocyclic inhibitors o ...
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Bioorg. Med. Chem. Lett.
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Chappell
Insights to substrate binding ...
West Nile virus
J. Biol. Chem.
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Breiman
A hepatitis C virus (HCV) NS3/ ...
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2006
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Peptide inhibitors of West Nil ...
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Cheng
Inhibition of dsRNA-induced si ...
Hepacivirus C
Proc. Natl. Acad. Sci. USA
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2006
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667671
Hamill
Enzymatic characterization of ...
Hepacivirus C
Biochemistry
44
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2005
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Chappell
Site-directed mutagenesis and ...
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Lin
In vitro studies of cross-resi ...
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2005
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5
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2
5
3
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1
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Chambers
Yellow fever virus NS2B-NS3 pr ...
Yellow fever virus
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2005
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670679
Li
Hepatitis C virus protease NS3 ...
Hepacivirus C
Proc. Natl. Acad. Sci. USA
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17717-17722
2005
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Liu
Hepatitis C NS3 protease inhib ...
Hepacivirus C
Arch. Biochem. Biophys.
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207-216
2004
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1
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1
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1
1
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652513
Richer
Serpin mechanism of hepatitis ...
Hepacivirus C
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2004
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Wyss
Non-peptidic small-molecule in ...
Hepacivirus C
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2004
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10
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652757
Rancourt
Peptide-based inhibitors of th ...
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J. Med. Chem.
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2004
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8
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1
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667187
Pacini
Reporter substrates for assess ...
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2004
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2
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667770
Poliakov
Structure-activity relationshi ...
Hepacivirus C
Biochim. Biophys. Acta
1672
51-59
2004
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7
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7
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669290
Nall
Enzymatic characterization and ...
West Nile virus
J. Biol. Chem.
279
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2004
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1
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4
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4
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669772
Bailey
Novel azapeptide inhibitors of ...
Hepacivirus C
J. Med. Chem.
47
3788-3799
2004
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1
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669774
Llinas-Brunet
A systematic approach to the o ...
Hepacivirus C
J. Med. Chem.
47
6584-6594
2004
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2
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1
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20
2
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-
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-
-
-
-
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-
-
-
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669971
Goudreau
Potent inhibitors of the hepat ...
Hepacivirus C
J. Org. Chem.
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2004
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4
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-
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650228
Liu
Investigating the origin of th ...
Hepacivirus C
Biochemistry
42
8862-8869
2003
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4
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7
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1
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652747
Colarusso
Phenethyl amides as novel nonc ...
Hepacivirus C
J. Med. Chem.
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345-348
2003
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26
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653406
Slater
Pyrrolidine-5,5-trans-lactams. ...
Hepacivirus C
Org. Lett.
5
4627-4630
2003
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20
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667915
Johansson
Acyl sulfonamides as potent pr ...
Hepacivirus C
Bioorg. Med. Chem.
11
2551-2568
2003
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-
-
-
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6
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1
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6
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6
6
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-
650158
Ingallinella
Prime site binding inhibitors ...
Hepacivirus C
Biochemistry
41
5483-5492
2002
1
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4
-
2
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2
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1
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4
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2
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650563
Priestley
P1 Phenethyl peptide boronic a ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
12
3199-3202
2002
-
-
-
-
-
-
1
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2
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-
-
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650830
Archer
Hepatitis C virus NS3 protease ...
Hepacivirus C
Chem. Biol.
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79-92
2002
1
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-
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1
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1
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1
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-
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-
-
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653748
Poliakov
Expression and purification of ...
Hepacivirus C
Protein Expr. Purif.
25
363-371
2002
-
-
1
-
-
-
5
-
-
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1
-
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1
-
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1
-
-
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1
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5
-
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1
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5
5
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1
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1
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1
-
-
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-
-
-
-
-
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653795
Casbarra
The effect of prime-site occup ...
Hepacivirus C
Protein Sci.
11
2102-2112
2002
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-
-
-
-
-
5
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2
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4
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649564
Kasai
Inhibition of the Hepatitis C ...
Hepacivirus C
Biochem. Biophys. Res. Commun.
281
416-424
2001
-
-
-
-
-
-
1
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3
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1
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1
1
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-
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-
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-
650070
Koch
Role of charged residues in th ...
Hepacivirus C
Biochemistry
40
631-640
2001
-
-
-
-
8
-
1
9
-
-
-
1
-
2
-
-
-
-
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-
-
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5
-
-
-
-
14
-
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-
9
-
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8
-
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1
9
9
-
-
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1
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-
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-
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5
-
-
-
-
14
-
-
-
-
-
-
-
-
-
-
651286
Mak
Reconstitution of hepatitis C ...
Hepacivirus C
FEBS Lett.
503
13-18
2001
-
-
1
-
2
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3
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-
-
-
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-
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-
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-
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652839
McCoy
Solution structure and dynamic ...
Hepacivirus C
J. Mol. Biol.
305
1099-1110
2001
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-
-
-
-
-
-
-
-
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1
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1
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1
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-
-
-
-
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-
-
-
-
-
-
-
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-
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652993
Poupart
Solid-phase synthesis of pepti ...
Hepacivirus C
J. Org. Chem.
66
4743-4751
2001
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-
-
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1
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33
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33
34
-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
653846
Beyer
Effect of naturally occurring ...
Hepacivirus C
Proteins Struct. Funct. Genet.
43
82-88
2001
-
-
-
-
6
-
11
-
-
-
-
-
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1
-
-
1
-
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-
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2
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-
-
-
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-
58
-
-
-
-
-
-
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6
-
-
11
58
-
-
-
-
-
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-
-
1
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-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649548
Butkiewicz
Hepatitis C NS3 protease: rest ...
Hepacivirus C
Biochem. Biophys. Res. Commun.
267
278-282
2000
1
-
-
-
-
-
-
-
-
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1
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1
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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649558
Hwang
The RNA aptamer-binding site o ...
Hepacivirus C
Biochem. Biophys. Res. Commun.
279
557-562
2000
-
-
-
-
-
-
3
-
-
-
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1
-
1
-
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-
-
-
-
-
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1
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-
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-
-
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-
-
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3
-
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-
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1
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-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649931
Ingallinella
Optimization of the P'-region ...
Hepacivirus C
Biochemistry
39
12898-12906
2000
-
-
-
-
-
-
5
-
-
-
-
-
-
2
-
-
-
-
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-
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5
-
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5
5
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649956
Narjes
alpha-Ketoacids are potent slo ...
Hepacivirus C
Biochemistry
39
1849-1861
2000
-
-
-
-
-
-
5
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
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5
4
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652087
Di Marco
Inhibition of the hepatitis C ...
Hepacivirus C
J. Biol. Chem.
275
7152-7157
2000
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1
-
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2
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2
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-
-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
-
1
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-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
81435
Sardana
An uniquely purified HCV NS3 p ...
Hepacivirus C
Protein Expr. Purif.
16
440-447
1999
1
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1
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-
-
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4
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1
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1
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1
3
1
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4
-
-
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-
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1
-
1
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-
-
-
-
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4
-
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1
-
-
-
-
1
-
-
-
1
3
1
-
-
-
4
-
-
-
-
-
-
-
-
-
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81437
Cicero
Structural characterization of ...
Hepacivirus C
J. Mol. Biol.
289
385-396
1999
1
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2
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-
-
-
-
-
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5
-
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1
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-
-
-
-
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5
5
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-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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81438
Bianchi
Conformational changes in huma ...
Hepacivirus C
Biochemistry
38
13844-13852
1999
-
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1
-
-
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7
-
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1
1
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1
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1
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-
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1
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-
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7
-
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1
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7
7
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1
1
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-
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1
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1
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-
-
-
-
-
-
-
-
-
-
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81439
Llinas-Brunet
Peptide-based inhibitors of th ...
Hepacivirus C
Bioorg. Med. Chem. Lett.
8
1713-1718
1998
1
1
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3
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1
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3
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1
1
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-
-
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-
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3
3
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-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
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-
-
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81440
Dimasi
Engineering, characterization ...
Hepacivirus C
Protein Eng.
11
1257-1265
1998
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1
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1
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1
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7
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-
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1
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1
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1
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8
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-
-
-
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-
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1
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-
-
-
1
-
-
-
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7
-
-
-
-
-
-
-
-
-
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81441
Taremi
Construction, expression, and ...
Hepacivirus C
Protein Sci.
7
2143-2149
1998
-
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1
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1
-
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3
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-
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1
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1
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1
1
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-
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3
1
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-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
3
-
-
-
-
-
-
-
1
-
-
-
1
1
-
-
-
-
3
1
-
-
-
-
-
-
-
-
-
81442
Steinkuhler
Product inhibition of the hepa ...
Hepacivirus C
Biochemistry
37
8899-8905
1998
-
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3
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4
2
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1
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1
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3
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-
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-
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-
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-
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-
-
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-
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3
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4
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2
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1
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-
-
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3
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-
-
-
-
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-
-
-
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81443
G¦nther
[Clarifying the crystal struct ...
Hepacivirus C
Z. Gastroenterol.
35
1119-1121
1997
-
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1
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-
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1
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-
-
-
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-
-
-
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-
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-
-
1
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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81444
Markland
Purification and characterizat ...
Hepacivirus C
J. Gen. Virol.
78
39-43
1997
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1
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1
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1
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-
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-
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-
-
-
1
-
-
-
-
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4
-
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-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
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-
-
81445
Wilkinson
Characterisation of an HCV NS3 ...
Hepacivirus C
Biochem. Soc. Trans.
25
S624
1997
2
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-
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1
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3
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1
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2
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-
-
-
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-
-
-
-
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-
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3
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-
-
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1
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-
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81446
Landro
Mechanistic role of an NS4A pe ...
Hepacivirus C
Biochemistry
36
9340-9348
1997
1
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4
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6
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81432
Kim
Crystal structure of the hepat ...
Hepacivirus C
Cell
87
343-355
1996
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1
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81433
Love
The crystal structure of hepat ...
Hepacivirus C
Cell
87
331-342
1996
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1
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1
1
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1
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1
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1
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1
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1
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1
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3
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81449
Mori
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1995
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