Compounds > gs-9451
Page last updated: 2024-11-13

gs-9451

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID25167947
CHEMBL ID2013174
SCHEMBL ID10082460
SCHEMBL ID16241357
MeSH IDM0575132

Synonyms (26)

Synonym
kgd958x2b9 ,
unii-kgd958x2b9
1098189-15-1
gs 9451
gs9451
vedroprevir [usan:inn]
bdbm50379653
vedroprevir (usan)
D10408
CHEMBL2013174 ,
gs-9451 ,
vedroprevir
vedroprevir [usan]
n-(((1r,3r,5s)-bicyclo(3.1.0)hex-3-yloxy)carbonyl(-3-methyl-l-valyl-(4r)-4-((8-chloro-2-(2-((1-methylethyl)amino)thiazol-4-yl(-7-(2-(morpholin-4-yl)ethoxy)quinolin-4-yl)oxy)-l-prolyl-(1r,2r)-1-amino-2-ethylcyclopropanecarboxylic acid
vedroprevir [inn]
vedroprevir [who-dd]
(1r,2r)-1-[[(2s,4r)-1-[(2s)-2-[[(1s,5r)-3-bicyclo[3.1.0]hexanyl]oxycarbonylamino]-3,3-dimethyl-butanoyl]-4-[[8-chloro-2-[2-(isopropylamino)thiazol-4-yl]-7-(2-morpholinoethoxy)-4-quinolyl]oxy]pyrrolidine-2-carbonyl]amino]-2-ethyl-cyclopropanecarboxylic aci
SCHEMBL10082460
1310824-24-8
SCHEMBL16241357
cyclopropanecarboxylic acid, n-[[(1a,3b,5a)-bicyclo[3.1.0]hex-3-yloxy]carbonyl]-3-methyl-l-valyl-(4r)-4-[[8-chloro-2-[2-[(1-methylethyl)amino]-4-thiazolyl]-7-[2-(4-morpholinyl)ethoxy]-4-quinolinyl]oxy]-l-prolyl-1-amino-2-ethyl-, (1r,2r)-
DB12037
(1r,2r)-1-((2s,4r)-1-((2s)-2-(((((1r,5s)-bicyclo[3.1.0]hexan-3-yl)oxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((8-chloro-2-(2-(isopropylamino)thiazol-4-yl)-7-(2-morpholinoethoxy)quinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-ethylcyclopropane-1-carboxylic
(1r,2r)-1-[[(2s,4r)-1-[(2s)-2-[[(1r,5s)-3-bicyclo[3.1.0]hexanyl]oxycarbonylamino]-3,3-dimethylbutanoyl]-4-[8-chloro-7-(2-morpholin-4-ylethoxy)-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxypyrrolidine-2-carbonyl]amino]-2-ethylcyclopropane-1-ca
Q27282236
AKOS040754345

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" GS-9451 showed good oral bioavailability in all three species tested."( Preclinical characterization of the novel hepatitis C virus NS3 protease inhibitor GS-9451.
Cheng, G; Corsa, AC; Delaney, WE; Kim, CU; Krawczyk, S; Mo, H; Pakdaman, R; Peng, B; Qi, X; Robinson, M; Shen, M; Sheng, XC; Tay, C; Tian, Y; Wang, Y; Yang, C; Yang, H, 2014)		1.54

Dosage Studied

ExcerptRelevanceReference
" Patients were randomized to 3 days of once-daily dosing with placebo (n=8) or GS-9451 60 mg (n=8 genotype 1a), 200 mg (n=8 genotype 1a; n=8 genotype 1b) or 400 mg (n=9 genotype 1a)."( A Phase I, randomized, placebo-controlled, 3-day, ascending-dose study of GS-9451, an NS3/4A protease inhibitor, in genotype 1 hepatitis C patients.
Delaney, W; Demicco, MP; Gordon, SC; Hill, JM; Lawitz, EJ; Marbury, T; Mathias, A; McHutchison, JG; Mo, H; Moorehead, L; Rodriguez-Torres, M; Yang, J, 2013)		0.85
"No patients interrupted or discontinued dosing because of an adverse event."( A Phase I, randomized, placebo-controlled, 3-day, ascending-dose study of GS-9451, an NS3/4A protease inhibitor, in genotype 1 hepatitis C patients.
Delaney, W; Demicco, MP; Gordon, SC; Hill, JM; Lawitz, EJ; Marbury, T; Mathias, A; McHutchison, JG; Mo, H; Moorehead, L; Rodriguez-Torres, M; Yang, J, 2013)		0.62
"Treatment with GS-9669, a novel nonnucleoside inhibitor (site II) of hepatitis C virus (HCV) nonstructural 5B (NS5B) polymerase, resulted in significant antiviral activity in HCV genotype (GT) 1 patients dosed at 50 and 500 mg once daily (QD) and at 50, 100, and 500 mg twice daily (BID) for 3 days."( Clinical and in vitro resistance to GS-9669, a thumb site II nonnucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Delaney, W; Dvory-Sobol, H; Lawitz, EJ; Mabery, E; McHutchison, J; Miller, MD; Mo, H; Skurnac, T; Svarovskaia, ES; Voitenleitner, C, 2014)		0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Multidrug resistance-associated protein 1 Homo sapiens (human)IC50 (µMol)14.90000.00153.71109.6600AID654820
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)12.00002.41006.343310.0000AID654821
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)1.40000.00401.966610.0000AID654822
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (36)

Processvia Protein(s)Taxonomy
leukotriene metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
response to xenobiotic stimulusMultidrug resistance-associated protein 1 Homo sapiens (human)
cobalamin transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid biosynthetic processMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to oxidative stressMultidrug resistance-associated protein 1 Homo sapiens (human)
heme catabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transportMultidrug resistance-associated protein 1 Homo sapiens (human)
phospholipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
positive regulation of inflammatory responseMultidrug resistance-associated protein 1 Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cell chemotaxisMultidrug resistance-associated protein 1 Homo sapiens (human)
transepithelial transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cyclic nucleotide transportMultidrug resistance-associated protein 1 Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 1 Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to amyloid-betaMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
ATP bindingMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type vitamin B12 transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled lipid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basal plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
lateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
extracellular exosomeMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (49)

Assay IDTitleYearJournalArticle
AID1552078Binding affinity to HCV NS3/4a protease assessed as compound-protein adduct formation per mg protein using radiolabelled compound2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi
AID654822Inhibition of BCRP2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654815Selectivity for hepatitis C virus NS3/4A protease over human proteinase 32012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654780Inhibition of Hepatitis C virus genotype 1b NS3/4A protease2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654802Half life in cynomolgus monkey at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654796Clearance in rat at 1 mg/kg, iv and 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654787AUC in dog at 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654810Fraction unbound in human plasma2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654795AUC in rat at 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654813Selectivity for hepatitis C virus NS3/4A protease over human cathepsin D2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654817Inhibition of cytochrome P450 up to 25 uM2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654797Volume of distribution at steady state in rat at 1 mg/kg, iv and 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654823Antiviral activity against Hepatitis C virus genotype 1a infected in human assessed as log decrease in viral RNA level at 60 mg, po for 3 days2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654781Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh cells by luciferase reporter gene based replicon assay2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654820Inhibition of MRP12012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654807Cmax in cynomolgus monkey at 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654816Selectivity for hepatitis C virus NS3/4A protease over human leukocyte elastase2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654788Clearance in dog at 1 mg/kg, iv and 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654791Cmax in dog at 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654801Half life in rat microsomes2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654785Permeability from basolateral to apical side in human Caco2 cells2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654825Antiviral activity against Hepatitis C virus genotype 1a infected in human assessed as log decrease in viral RNA level at 400 mg, po for 3 days2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654789Volume of distribution at steady state in dog at 1 mg/kg, iv and 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654803AUC in cynomolgus monkey at 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654805Volume of distribution at steady state in cynomolgus monkey at 1 mg/kg, iv and 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654809Half life in cynomolgus monkey microsomes2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654790Oral bioavailability in dog at 4 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654808Fraction unbound in cynomolgus monkey plasma2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654798Oral bioavailability in rat at 4 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654793Half life in dog microsomes2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654818Inhibition of human Erg up to 25 uM2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654792Fraction unbound in dog plasma2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654786Half life in dog at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654827Plasma concentration in human at 300 mg/kg after 24 hrs2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654782Thermodynamic solubility of the compound at pH 7.32012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654783Thermodynamic solubility of the compound at pH 2.22012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654819Inhibition of p-glycoprotein2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654800Fraction unbound in rat plasma2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654824Antiviral activity against Hepatitis C virus genotype 1a infected in human assessed as log decrease in viral RNA level at 200 mg, po for 3 days2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654794Half life in rat at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654799Cmax in rat at 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654826Elimination half life in human at 10 to 1000 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654812Drug excretion in rat bile at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654784Permeability from apical to basolateral side in human Caco2 cells2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654814Selectivity for hepatitis C virus NS3/4A protease over human cathepsin L2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654821Inhibition of MRP22012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654811Half life in human microsomes2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654804Clearance in cynomolgus monkey at 1 mg/kg, iv and 4 mg/kg, po2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
AID654806Oral bioavailability in cynomolgus monkey at 4 mg/kg2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's17 (100.00)24.3611
2020's0 (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: 16.32

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.

MetricThis Compound (vs All)
Research Demand Index16.32 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (64.71%)5.53%
Reviews2 (11.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (23.53%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
uridine monophosphate
Uridine Monophosphate: 5'-Uridylic acid. A uracil nucleotide containing one phosphate group esterified to the sugar moiety in the 2', 3' or 5' position.. uridine 5'-monophosphate : A pyrimidine ribonucleoside 5'-monophosphate having uracil as the nucleobase.		8.4164pyrimidine ribonucleoside 5'-monophosphate;
uridine 5'-phosphate		Escherichia coli metabolite;
human metabolite;
mouse metabolite
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		8.1676mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
ribavirin
Rebetron: Rebetron is tradename		8.54741-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
biln 2061
BILN 2061: a macrocyclic NS3 protease inhibitor and antiviral agent; structure in first source		3.4611
danoprevir
[no description available]		2.2110
bms-650032
asunaprevir: an NS3 protease inhibitor against hepatitis C virus		2.2110oligopeptide
tegobuvir
tegobuvir: a non-structural protein 5B polymerase inhibitor		3.8921
mk-7009
vaniprevir: inhibits hepatitis C virus NS3/4a protease. vaniprevir : An azamacrocyclic compound that is a hepatitis C virus (HCV) NS3/4A protease inhibitor which is approved for the treatment of hepatitis C virus infections in Japan.		2.2110azamacrocycle;
carbamate ester;
cyclopropanes;
N-sulfonylcarboxamide;
pyrrolidinecarboxamide		antiviral drug;
hepatitis C protease inhibitor
gs-9256
GS-9256: has antiviral activity; structure in first source		3.5820
simeprevir
[no description available]		2.2110azamacrocycle;
lactam
bi 201335
faldaprevir: inhibits hepatitis C virus NS3 protease		2.2110
grazoprevir
grazoprevir: has antiviral activity; component of Zepatier. grazoprevir : An azamacrocyclic compound that is a hepatitis C protease inhibitor used in combination with elbasvir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults.		2.2110aromatic ether;
azamacrocycle;
carbamate ester;
cyclopropanes;
lactam;
N-sulfonylcarboxamide;
quinoxaline derivative		antiviral drug;
hepatitis C protease inhibitor;
hepatoprotective agent
abt-450
paritaprevir: inhibits HCV NS3 protease. paritaprevir : An azamacrocycle which is used which is in combination with dasabuvir sodium hydrate, ombitasvir and ritonavir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.2110
sofosbuvir
Sofosbuvir: A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.. sofosbuvir : A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.		9.6297isopropyl ester;
L-alanyl ester;
nucleotide conjugate;
organofluorine compound;
phosphoramidate ester		antiviral drug;
hepatitis C protease inhibitor;
prodrug
gs-9669
[no description available]		8.1676
ledipasvir
ledipasvir : A benzimidazole derivative that is used in combination with sofosbuvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.		8.75108azaspiro compound;
benzimidazole;
bridged compound;
carbamate ester;
carboxamide;
fluorenes;
imidazoles;
L-valine derivative;
N-acylpyrrolidine;
organofluorine compound		antiviral drug;
hepatitis C protease inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		07.7364
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		07.7364
Chronic Hepatitis C
[description not available]		09.75118
Hepatitis C, Chronic
INFLAMMATION of the LIVER in humans that is caused by HEPATITIS C VIRUS lasting six months or more. Chronic hepatitis C can lead to LIVER CIRRHOSIS.		09.75118
Cirrhosis, Liver
[description not available]		03.5111
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		03.5111
Dyslipidemia
[description not available]		03.5111
Co-infection
[description not available]		03.5111
HIV Coinfection
[description not available]		03.5111
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		03.5111
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		03.5111
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		03.5111