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Literature summary for 3.4.21.98 extracted from

  • Clarke, M.O.; Chen, X.; Cho, A.; Delaney, W.E.; Doerffler, E.; Fardis, M.; Ji, M.; Mertzman, M.; Pakdaman, R.; Pyun, H.J.; Rowe, T.; Yang, C.Y.; Sheng, X.C.; Kim, C.U.
    Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease (2011), Bioorg. Med. Chem. Lett., 21, 3568-3572.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(ethyl)phosphinic acid
-
Hepacivirus C
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(methyl)phosphinic acid
-
Hepacivirus C
(2R,6R,12Z,13aR,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-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-14-carboxylic acid
-
Hepacivirus C
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(4-methoxybenzyl)phosphinic acid
-
Hepacivirus C
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(isopropyl)phosphinic acid
-
Hepacivirus C
(R)-((1S,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(phenyl)phosphinic acid
-
Hepacivirus C
(R)-(4-chlorobenzyl)((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
Hepacivirus C
(R)-benzyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
Hepacivirus C
(R)-butyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
Hepacivirus C
(S)-((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
Hepacivirus C
(S)-((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-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]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
Hepacivirus C
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
Hepacivirus C
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-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]diazacyclopentadecin-14-yl)phosphinic acid
-
Hepacivirus C
(S)-benzyl((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
Hepacivirus C
(S)-benzyl((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-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]diazacyclopentadecin-14-yl)phosphinic acid
-
Hepacivirus C
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3R)-2-carboxy-3-ethenylcyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
-
Hepacivirus C
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3S)-2-ethenyl-3-phosphonocyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
-
Hepacivirus C
[(2R,6R,12Z,13aS,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-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]diazacyclopentadecin-14-yl]phosphonic acid
-
Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
-
-
-

Synonyms

Synonyms Comment Organism
NS3 protease
-
Hepacivirus C

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000009
-
pH and temperature not specified in the publication Hepacivirus C N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3S)-2-ethenyl-3-phosphonocyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
0.000001
-
pH and temperature not specified in the publication Hepacivirus C (2R,6R,12Z,13aR,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-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-14-carboxylic acid
0.000001
-
pH and temperature not specified in the publication Hepacivirus C [(2R,6R,12Z,13aS,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-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]diazacyclopentadecin-14-yl]phosphonic acid
0.000001
-
pH and temperature not specified in the publication Hepacivirus C (S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-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]diazacyclopentadecin-14-yl)phosphinic acid
0.000003
-
pH and temperature not specified in the publication Hepacivirus C N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3R)-2-carboxy-3-ethenylcyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
0.000003
-
pH and temperature not specified in the publication Hepacivirus C (S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
0.000003
-
pH and temperature not specified in the publication Hepacivirus C (S)-benzyl((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-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]diazacyclopentadecin-14-yl)phosphinic acid
0.000003
-
pH and temperature not specified in the publication Hepacivirus C (S)-((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-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]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
0.000006
-
pH and temperature not specified in the publication Hepacivirus C (S)-benzyl((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
0.000006
-
pH and temperature not specified in the publication Hepacivirus C ((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(methyl)phosphinic acid
0.000006
-
pH and temperature not specified in the publication Hepacivirus C (R)-(4-chlorobenzyl)((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
0.000006
-
pH and temperature not specified in the publication Hepacivirus C (R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(4-methoxybenzyl)phosphinic acid
0.000008
-
pH and temperature not specified in the publication Hepacivirus C ((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(ethyl)phosphinic acid
0.000008
-
pH and temperature not specified in the publication Hepacivirus C (R)-butyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
0.000009
-
pH and temperature not specified in the publication Hepacivirus C (R)-benzyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
0.000044
-
pH and temperature not specified in the publication Hepacivirus C (R)-((1S,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(phenyl)phosphinic acid
0.000086
-
pH and temperature not specified in the publication Hepacivirus C (R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(isopropyl)phosphinic acid