bi 201335 profile

faldaprevir: inhibits hepatitis C virus NS3 protease [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	42601552
CHEMBL ID	1241348
SCHEMBL ID	222429
MeSH ID	M0550196

Synonym
(1r,2s)-1-((2s,4r)-4-(8-bromo-2-(2-isobutyramidothiazol-4-yl)-7-methoxyquinolin-4-yloxy)-1-((s)-2-(cyclopentyloxycarbonylamino)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-2-vinylcyclopropanecarboxylic acid
bdbm50336545
bi-201335
n-[(cyclopentyloxy)carbonyl]-3-methyl-l-valyl-(4r)-4-[(8-bromo-7-methoxy-2-{2-[(2-methylpropanoyl)amino]-1,3-thiazol-4-yl}quinolin-4-yl)oxy]-n-[(1r,2s)-1-carboxy-2-ethenylcyclopropyl]-l-prolinamide
l4t ,
bi201335
faldaprevir
bi 201335
CHEMBL1241348 ,
faldaprevir [usan:inn]
n-((cyclopentyloxy)carbonyl)-3-methylvalyl-4-((8-bromo-7-methoxy-2-(2-((2-methylpropanoyl)amino)-1,3-thiazol-4-yl)quinolin-4-yl)oxy)-n-(1-carboxy-2-ethenylcyclopropyl)prolinamide
801283-95-4
cyclopropanecarboxylic acid, n-((cyclopentyloxy)carbonyl)-3-methyl-l-valyl- (4r)-4-((8-bromo-7-methoxy-2-(2-((2-methyl-1-oxopropyl)amino)-4-thiazolyl)-4-quinolinyl)oxy)-l-prolyl-1-amino-2-ethenyl-, (1r,2s)-
unii-958x4j301a
958x4j301a ,
SCHEMBL222429
(1r,2s)-1-[[(2s,4r)-4-[[8-bromo-7-methoxy-2-[2-(2-methylpropanoylamino)thiazol-4-yl]-4-quinolyl]oxy]-1-[(2s)-2-(cyclopentoxycarbonylamino)-3,3-dimethyl-butanoyl]pyrrolidine-2-carbonyl]amino]-2-vinyl-cyclopropanecarboxylic acid
faldaprevir [who-dd]
(1r,2s)-1-((2s,4r)-4-((8-bromo-7-methoxy-2-(2-(2-methylpropanamido)-1,3-thiazol-4-yl)quinolin-4-yl)oxy)-1-((2s)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-2-ethenylcyclopropane-1-carboxylic acid
faldaprevir [usan]
faldaprevir [inn]
DB11808
(1r,2s)-1-((2s,4r)-4-((8-bromo-2-(2-isobutyramidothiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-1-((s)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-2-vinylcyclopropane-1-carboxylic acid
Q15408404
(1r,2s)-1-[[(2s,4r)-4-[8-bromo-7-methoxy-2-[2-(2-methylpropanoylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy-1-[(2s)-2-(cyclopentyloxycarbonylamino)-3,3-dimethylbutanoyl]pyrrolidine-2-carbonyl]amino]-2-ethenylcyclopropane-1-carboxylic acid
CS-0003827
HY-15256
AKOS040744413

Excerpt	Reference	Relevance
"BI 201335 is a hepatitis C virus (HCV) NS3-NS4A (NS3 coexpressed with NS4A) protease inhibitor that has been shown to have potent clinical antiviral activity. "	( Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease. Amad, M; Bethell, RC; Bolger, G; Cordingley, MG; Duan, J; Garneau, M; Kukolj, G; Lagacé, L; Llinàs-Brunet, M; Thibeault, D; White, PW, 2010)	2.09

Excerpt	Reference	Relevance
" There was one serious adverse event, which was not considered to be treatment related."	( Safety and efficacy of faldaprevir with pegylated interferon alfa-2a and ribavirin in Japanese patients with chronic genotype-1 hepatitis C infection. Kuboki, M; Nishiguchi, S; Omata, M; Sakai, Y; Sakamoto, W; Steinmann, G; Tsuda, Y; Tsunematsu, S; Urano, Y, 2014)	0.4
" Overall, 5/8 (63%) subjects with normal renal function and 20/24 (83%) subjects with renal impairment reported adverse events, with gastrointestinal events being the most common."	( Pharmacokinetics, safety, and tolerability of faldaprevir in patients with renal impairment. Elgadi, M; Halabi, A; Huang, F; Lang, B; Moschetti, V; Petersen-Sylla, M; Yong, CL, 2015)	0.42
" The most frequent adverse events in patients with/without cirrhosis were gastrointestinal and skin events, which were mostly mild or moderate in intensity."	( Efficacy and safety of faldaprevir, deleobuvir, and ribavirin in treatment-naive patients with chronic hepatitis C virus infection and advanced liver fibrosis or cirrhosis. Angus, P; Asselah, T; Böcher, W; Bourlière, M; Bronowicki, JP; Buti, M; Gallivan, JP; Gane, EJ; Lohse, AW; Manns, M; Mensa, FJ; Müllhaupt, B; Roberts, S; Sabo, JP; Schuchmann, M; Soriano, V; Stern, JO; Stickel, F; Voss, F; Zeuzem, S, 2015)	0.42

Excerpt	Reference	Relevance
" Serial blood samples were taken for pharmacokinetic analysis."	( Effect of steady-state faldaprevir on the pharmacokinetics of steady-state methadone and buprenorphine-naloxone in subjects receiving stable addiction management therapy. Adeniji, A; Elgadi, M; Huang, F; Joseph, D; Riesenberg, RR; Schobelock, MJ; Vince, BD; Webster, LR, 2015)	0.42
" Median t1/2 (terminal half-life in plasma at steady state) values were prolonged for both EE (2."	( Effect of the hepatitis C virus protease inhibitor faldaprevir on the pharmacokinetics of an oral contraceptive containing ethinylestradiol and levonorgestrel in healthy female volunteers. Elgadi, M; Huang, F; Lang, B; Sabo, JP, 2015)	0.42

Excerpt	Reference	Relevance
" Four hundred and twenty-nine HCV genotype (GT)-1 treatment-naïve patients without cirrhosis were randomized 1:1:2:2 to receive 24 weeks of pegylated interferon alfa-2a and ribavirin (PegIFN/RBV) in combination with placebo, faldaprevir 120 mg QD with 3 days of PegIFN/RBV lead-in (LI), 240 mg QD with LI, or 240 mg QD without LI, followed by an additional 24 weeks of PegIFN/RBV."	( Faldaprevir combined with pegylated interferon alfa-2a and ribavirin in treatment-naïve patients with chronic genotype 1 HCV: SILEN-C1 trial. Asselah, T; Bessone, F; Böcher, WO; Datsenko, Y; Fainboim, H; Ferenci, P; Heo, J; Kukolj, G; Lalezari, J; Leggett, B; Mauss, S; Nehmiz, G; Scherer, J; Steinmann, GG; Stern, JO; Sulkowski, MS, 2013)	0.39

Excerpt	Reference	Relevance
"6 mL/min/kg in rat, monkey and dog respectively, with a corresponding oral bioavailability of 29."	( Cross-species absorption, metabolism, distribution and pharmacokinetics of BI 201335, a potent HCV genotype 1 NS3/4A protease inhibitor. Amad, M; Bethell, RC; Bolger, G; Cordingley, MG; De Marte, J; Duan, J; Garneau, M; Jutras, M; Llinàs-Brunet, M; Montpetit, H; Otis, F; Rhéaume, M; White, PW; Yong, CL, 2012)	0.61
"This study was conducted to investigate the effect of food and coadministration of omeprazole on the relative bioavailability (BA) of faldaprevir (FDV)."	( Investigation of the effect of food and omeprazole on the relative bioavailability of a single oral dose of 240 mg faldaprevir, a selective inhibitor of HCV NS3/4 protease, in an open-label, randomized, three-way cross-over trial in healthy participants. Elgadi, M; Gießmann, T; Huang, F; Lang, B; Wu, J, 2016)	0.43

Excerpt	Relevance	Reference
" The sustained virologic response 12 weeks after the completion of therapy did not differ significantly according to treatment duration or dosage among ribavirin-containing regimens."	( Faldaprevir and deleobuvir for HCV genotype 1 infection. Asselah, T; Böcher, WO; Bourlière, M; Bronowicki, JP; Buti, M; Gallivan, JP; Gane, EJ; Kukolj, G; Lohse, AW; Mensa, FJ; Müllhaupt, B; Roberts, SK; Schuchmann, M; Soriano, V; Stern, JO; Vinisko, R; Zeuzem, S, 2013)	0.39
" Although individual data showed moderate variability in the exposures between subjects and treatments, there was no evidence of symptoms of opiate overdose or withdrawal either during the coadministration of faldaprevir with methadone or buprenorphine-naloxone or after faldaprevir dosing was stopped."	( Effect of steady-state faldaprevir on the pharmacokinetics of steady-state methadone and buprenorphine-naloxone in subjects receiving stable addiction management therapy. Adeniji, A; Elgadi, M; Huang, F; Joseph, D; Riesenberg, RR; Schobelock, MJ; Vince, BD; Webster, LR, 2015)	0.42
" dosing for 5 days."	( Investigation of the effect of food and omeprazole on the relative bioavailability of a single oral dose of 240 mg faldaprevir, a selective inhibitor of HCV NS3/4 protease, in an open-label, randomized, three-way cross-over trial in healthy participants. Elgadi, M; Gießmann, T; Huang, F; Lang, B; Wu, J, 2016)	0.43

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Genome polyprotein		Ki	0.0020	0.0000	0.0067	0.0300	AID1173945; AID1173956
Non-structural protein 4A		Ki	0.0020	0.0000	0.0067	0.0300	AID1173945; AID1173956
Cathepsin B	Homo sapiens (human)	IC50 (µMol)	26.0000	0.0002	1.8453	10.0000	AID575659
Neutrophil elastase	Homo sapiens (human)	IC50 (µMol)	30.0000	0.0063	2.0734	22.3780	AID575658
Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)	IC50 (µMol)	9.0000	9.0000	9.0000	9.0000	AID575882
Sterol O-acyltransferase 2	Rattus norvegicus (Norway rat)	IC50 (µMol)	2.4000	2.4000	2.4000	2.4000	AID575881
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
proteolysis	Cathepsin B	Homo sapiens (human)
thyroid hormone generation	Cathepsin B	Homo sapiens (human)
collagen catabolic process	Cathepsin B	Homo sapiens (human)
epithelial cell differentiation	Cathepsin B	Homo sapiens (human)
regulation of apoptotic process	Cathepsin B	Homo sapiens (human)
decidualization	Cathepsin B	Homo sapiens (human)
symbiont entry into host cell	Cathepsin B	Homo sapiens (human)
proteolysis involved in protein catabolic process	Cathepsin B	Homo sapiens (human)
cellular response to thyroid hormone stimulus	Cathepsin B	Homo sapiens (human)
proteolysis	Neutrophil elastase	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Neutrophil elastase	Homo sapiens (human)
response to yeast	Neutrophil elastase	Homo sapiens (human)
leukocyte migration involved in inflammatory response	Neutrophil elastase	Homo sapiens (human)
biosynthetic process of antibacterial peptides active against Gram-negative bacteria	Neutrophil elastase	Homo sapiens (human)
proteolysis	Neutrophil elastase	Homo sapiens (human)
intracellular calcium ion homeostasis	Neutrophil elastase	Homo sapiens (human)
response to UV	Neutrophil elastase	Homo sapiens (human)
extracellular matrix disassembly	Neutrophil elastase	Homo sapiens (human)
protein catabolic process	Neutrophil elastase	Homo sapiens (human)
response to lipopolysaccharide	Neutrophil elastase	Homo sapiens (human)
negative regulation of chemokine production	Neutrophil elastase	Homo sapiens (human)
negative regulation of interleukin-8 production	Neutrophil elastase	Homo sapiens (human)
positive regulation of interleukin-8 production	Neutrophil elastase	Homo sapiens (human)
defense response to bacterium	Neutrophil elastase	Homo sapiens (human)
positive regulation of MAP kinase activity	Neutrophil elastase	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Neutrophil elastase	Homo sapiens (human)
negative regulation of inflammatory response	Neutrophil elastase	Homo sapiens (human)
positive regulation of immune response	Neutrophil elastase	Homo sapiens (human)
negative regulation of chemotaxis	Neutrophil elastase	Homo sapiens (human)
pyroptosis	Neutrophil elastase	Homo sapiens (human)
neutrophil-mediated killing of gram-negative bacterium	Neutrophil elastase	Homo sapiens (human)
neutrophil-mediated killing of fungus	Neutrophil elastase	Homo sapiens (human)
positive regulation of leukocyte tethering or rolling	Neutrophil elastase	Homo sapiens (human)
phagocytosis	Neutrophil elastase	Homo sapiens (human)
acute inflammatory response to antigenic stimulus	Neutrophil elastase	Homo sapiens (human)
T cell mediated cytotoxicity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
negative regulation of T cell mediated cytotoxicity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
lymphangiogenesis	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
protein dephosphorylation	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
signal transduction	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
heart development	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
learning	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
memory	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
dephosphorylation	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calcium-ion regulated exocytosis	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
negative regulation of signaling	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
T cell differentiation	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
locomotion involved in locomotory behavior	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calcineurin-NFAT signaling cascade	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
response to cytokine	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulus	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
T cell proliferation	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
T cell activation	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
T cell homeostasis	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of DNA-templated transcription	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
regulation of synaptic plasticity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
axon extension	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
skeletal muscle fiber development	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
regulation of insulin secretion	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of calcineurin-NFAT signaling cascade	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calcineurin-mediated signaling	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of protein localization to nucleus	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
regulation of synaptic vesicle endocytosis	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of calcium ion import across plasma membrane	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
positive regulation of lysosome organization	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
negative regulation of calcium ion import across plasma membrane	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cysteine-type endopeptidase activity	Cathepsin B	Homo sapiens (human)
protein binding	Cathepsin B	Homo sapiens (human)
collagen binding	Cathepsin B	Homo sapiens (human)
peptidase activity	Cathepsin B	Homo sapiens (human)
cysteine-type peptidase activity	Cathepsin B	Homo sapiens (human)
proteoglycan binding	Cathepsin B	Homo sapiens (human)
protease binding	Neutrophil elastase	Homo sapiens (human)
transcription corepressor activity	Neutrophil elastase	Homo sapiens (human)
endopeptidase activity	Neutrophil elastase	Homo sapiens (human)
serine-type endopeptidase activity	Neutrophil elastase	Homo sapiens (human)
protein binding	Neutrophil elastase	Homo sapiens (human)
heparin binding	Neutrophil elastase	Homo sapiens (human)
peptidase activity	Neutrophil elastase	Homo sapiens (human)
cytokine binding	Neutrophil elastase	Homo sapiens (human)
protein serine/threonine phosphatase activity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calcium ion binding	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
protein binding	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calmodulin binding	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
myosin phosphatase activity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
enzyme binding	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
protein phosphatase 2B binding	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calmodulin-dependent protein phosphatase activity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
protein dimerization activity	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
collagen-containing extracellular matrix	Cathepsin B	Homo sapiens (human)
extracellular region	Cathepsin B	Homo sapiens (human)
extracellular space	Cathepsin B	Homo sapiens (human)
lysosome	Cathepsin B	Homo sapiens (human)
external side of plasma membrane	Cathepsin B	Homo sapiens (human)
apical plasma membrane	Cathepsin B	Homo sapiens (human)
endolysosome lumen	Cathepsin B	Homo sapiens (human)
melanosome	Cathepsin B	Homo sapiens (human)
perinuclear region of cytoplasm	Cathepsin B	Homo sapiens (human)
collagen-containing extracellular matrix	Cathepsin B	Homo sapiens (human)
extracellular exosome	Cathepsin B	Homo sapiens (human)
peptidase inhibitor complex	Cathepsin B	Homo sapiens (human)
ficolin-1-rich granule lumen	Cathepsin B	Homo sapiens (human)
extracellular space	Cathepsin B	Homo sapiens (human)
lysosome	Cathepsin B	Homo sapiens (human)
extracellular region	Neutrophil elastase	Homo sapiens (human)
extracellular space	Neutrophil elastase	Homo sapiens (human)
cytoplasm	Neutrophil elastase	Homo sapiens (human)
cytosol	Neutrophil elastase	Homo sapiens (human)
cell surface	Neutrophil elastase	Homo sapiens (human)
secretory granule	Neutrophil elastase	Homo sapiens (human)
azurophil granule lumen	Neutrophil elastase	Homo sapiens (human)
specific granule lumen	Neutrophil elastase	Homo sapiens (human)
phagocytic vesicle	Neutrophil elastase	Homo sapiens (human)
collagen-containing extracellular matrix	Neutrophil elastase	Homo sapiens (human)
extracellular exosome	Neutrophil elastase	Homo sapiens (human)
transcription repressor complex	Neutrophil elastase	Homo sapiens (human)
extracellular space	Neutrophil elastase	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
cytoplasm	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
cytosol	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
plasma membrane	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
calcineurin complex	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
protein serine/threonine phosphatase complex	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
Z disc	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
T-tubule	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
glutamatergic synapse	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
cytoplasm	Serine/threonine-protein phosphatase 2B catalytic subunit beta isoform	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID575834	Inhibition of human trypsin at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575805	Inhibition of human recombinant caspase-10 expressed in Escherichia coli at 10 uM by fluorimetry	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575833	Inhibition of human TACE at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575847	Inhibition of rat GABA-A receptor, agonist site at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1173956	Inhibition of HCV genotype 1b NS3/4A protease	2014	Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23	Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles.
AID575875	Inhibition of human neutral endopeptidase from HUV-EC-C cells at 10 uM by fluorimetry	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575789	AUC in monkey at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575652	Inhibition of HCV 1b NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575671	Clearance in dog liver microsomes	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575649	Inhibition of rat cNOS at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575876	Inhibition of rat calcium channel L-type, dihydropyridine site at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575851	Inhibition of human H1 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575819	Inhibition of human kallikrein at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575804	Inhibition of human caspase-9 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575878	Inhibition of rat GABA-A receptor, benzodiazepine central at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575862	Inhibition of rat 5-HT2A receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575641	Inhibition of rabbit ACE at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1645925	Antiviral activity against HCV genotype 1a	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	A review on HCV inhibitors: Significance of non-structural polyproteins.
AID575814	Inhibition of human chymase at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575640	Inhibition of rat 5-HT1 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID509556	Inhibition of HCV NS3 protease	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335).
AID1072927	Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells by subgenomic replicon-based luciferase assay	2014	ACS medicinal chemistry letters, Mar-13, Volume: 5, Issue:3	Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region.
AID575873	Inhibition of human serum elastase, neutrophil at 10 uM by fluorimetry	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575798	Inhibition of human caspase-3 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575854	Inhibition of human nicotinic acetylcholine receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575657	Inhibition of HCV 6a NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575650	Inhibition of mouse iNOS at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575645	Inhibition of human adenosine A1 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575675	Cmax in Sprague-Dawley rat at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575658	Inhibition of human leukocyte elastase after 60 mins fluorescence assay	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575861	Inhibition of human 5-HT1A receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575842	Inhibition of human dopamine receptor 2s at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575882	Inhibition of human PP2B	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575812	Inhibition of human cathepsin L at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575818	Inhibition of human factor 10a at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575799	Inhibition of human caspase-4 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1070543	Antiviral activity against Hepatitis C virus genotype 1b isolate Con1 harboring NS3 D168V mutant gene assessed as luciferase activity after 72 hrs by cell-based replicon assay	2014	Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5	Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.
AID575783	Cmax in monkey at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575844	Inhibition of human dopamine receptor 3 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575858	Inhibition of rat potassium channel-V at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575795	Inhibition of human calpain-1 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575843	Inhibition of human dopamine receptor 2L at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575839	Inhibition of rat calcium channel N-type at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575642	Inhibition of human ACE at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575664	Antiviral activity against HCV 2a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575860	Inhibition of human Thromboxane A2 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575859	Inhibition of rat Small conductance calcium-activated potassium channel at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575881	Inhibition of rat hapatic, acyl coA cholesterol acetyltransferase	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575856	Inhibition of rat potassium channel-A at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575841	Inhibition of human dopamine receptor 1 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575663	Antiviral activity against HCV 1b infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575824	Inhibition of human MMP-8 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1552078	Binding affinity to HCV NS3/4a protease assessed as compound-protein adduct formation per mg protein using radiolabelled compound	2019	Bioorganic & 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
AID575826	Inhibition of human MMP-13 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575660	Binding affinity to HCV 5a NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575667	Apparent permeability from basolateral to apical side in human Caco2 cells	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1173955	Antiviral activity against HCV genotype 1b	2014	Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23	Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles.
AID575872	Inhibition of human dopamine receptor 4.7 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575796	Inhibition of human caspase-1 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575654	Inhibition of HCV 2b NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575646	Inhibition of human adenosine A2A receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575813	Inhibition of human cathepsin X at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575661	Cytotoxicity activity against human HuH7 cells by MTT assay	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575838	Inhibition of human norepinephrine transporter at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575792	AUC (0 to infinity) in monkey at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575647	Inhibition of human PP2B at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1070542	Antiviral activity against Hepatitis C virus genotype 1a isolate H77 harboring NS3 R155K mutant gene assessed as luciferase activity after 72 hrs by cell-based replicon assay	2014	Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5	Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.
AID575794	Inhibition of human recombinant BACE-1 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575791	AUC (0 to infinity) in rat at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575877	Inhibition of rat calcium channel L-type, phenylalkylamine site at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575864	Inhibition of guinea pig 5-HT4 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575666	Apparent permeability from apical to basolateral side in human Caco2 cells	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575802	Inhibition of human caspase-7 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1070540	Permeability from apical to basolateral side of human Caco2 cells	2014	Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5	Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.
AID575786	Tmax in monkey at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575827	Inhibition of human MMP-14 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575831	Inhibition of human plasmin at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575845	Inhibition of human dopamine receptor 5 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575816	Inhibition of human elastase, leukocyte at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575803	Inhibition of human caspase-8 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575830	Inhibition of human tPA at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575863	Inhibition of rat 5-HT3 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575809	Inhibition of mouse recombinant cathepsin E at 10 uM by fluorimetry	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575836	Inhibition of human acetylcholinesterase at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575656	Inhibition of HCV 4a NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1173945	Inhibition of HCV genotype 1a NS3/4A protease using Ac-DED(Edans)EEAbu-psi[COO]ASK(Dabcyl)-NH2 as substrate by FRET assay	2014	Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23	Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles.
AID575648	Inhibition of rat PKC at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575869	Inhibition of guinea pig adenosine transporter at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575857	Inhibition of syrian hamster potassium channel-ATP at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575662	Antiviral activity against HCV 1a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575790	AUC in dog at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575673	Mean retention time in dog at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575644	Inhibition of rat adrenergic receptor Alpha-1at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575849	Inhibition of rat IP3 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575665	Antiviral activity against HCV 2a clone JFH1 infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575806	Inhibition of human cathepsin B at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575788	AUC in rat at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575653	Inhibition of HCV 2a NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575848	Inhibition of rat glycine receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1173954	Antiviral activity against HCV genotype 1a	2014	Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23	Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles.
AID575868	Inhibition of rat GABA B receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575669	Clearance in Sprague-Dawley rat liver microsomes	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575822	Inhibition of human MMP-3 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575815	Inhibition of human chymotrypsin at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575810	Inhibition of human cathepsin G at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575835	Inhibition of human tryptase at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575823	Inhibition of human MMP-7 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575820	Inhibition of human MMP-1 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575643	Inhibition of rat adrenergic receptor Alpha-2 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575855	Inhibition of rat opiate receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575651	Inhibition of HCV 1a NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575670	Clearance in monkey liver microsomes	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575846	Inhibition of rat glutamate receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1645926	Antiviral activity against HCV genotype 1b	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	A review on HCV inhibitors: Significance of non-structural polyproteins.
AID575832	Inhibition of rat neutral endopeptidase at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1070545	Antiviral activity against Hepatitis C virus genotype 1b isolate Con1 harboring wild type NS2-NS5B gene assessed as luciferase activity after 72 hrs by cell-based replicon assay	2014	Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5	Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.
AID575668	Clearance in human liver microsomes	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575880	Inhibition of mouse recombinant cathepsin E by fluorimetry	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575837	Inhibition of rat hapatic, acyl coA cholesterol acetyltransferase at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575655	Inhibition of HCV 3a NS3/4A protease	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575840	Inhibition of rat calcium channel L-type, benzothiazepine site at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575853	Inhibition of rat mAChR at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575784	Cmax in dog at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575787	Tmax in dog at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575865	Inhibition of human 5-HT6 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575674	Mean retention time in monkey at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575797	Inhibition of human caspase-2 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575871	Inhibition of human dopamine receptor 4.4 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID509557	Antiviral activity against HCV Con1 by cell based-luciferase reporter gene assay	2010	Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17	Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335).
AID1070541	Half life in human liver microsomes	2014	Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5	Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.
AID575825	Inhibition of human MMP-9 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575867	Inhibition of rat sodium channel site 2 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575874	Inhibition of human endothelin-converting enzyme at 10 uM by cerep assay	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575866	Inhibition of human 5-HT7 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575828	Inhibition of human neutral endopeptidase at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575800	Inhibition of human caspase-5 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575870	Inhibition of human dopamine receptor 4.2 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575829	Inhibition of human thrombin at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID1070544	Antiviral activity against Hepatitis C virus genotype 1a isolate H77 harboring wild type NS2-NS5B gene assessed as luciferase activity after 72 hrs by cell-based replicon assay	2014	Journal of medicinal chemistry, Mar-13, Volume: 57, Issue:5	Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution.
AID1072931	Inhibition of Hepatitis C virus genotype 1a full length NS3/2K-NS4A protease using Ac-DED(Edans)EEAbupsi[COO]ASK(Dabcyl)-NH2 as substrate incubated for 10 mins prior to substrate addition by FRET analysis	2014	ACS medicinal chemistry letters, Mar-13, Volume: 5, Issue:3	Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region.
AID575817	Inhibition of human factor 7a at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575672	Mean retention time in Sprague-Dawley rat at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575811	Inhibition of human cathepsin H at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575879	Inhibition of rat GABA-A receptor, chloride channel at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575850	Inhibition of human H2 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575821	Inhibition of human MMP-2 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575659	Inhibition of human CatB after 60 mins fluorescence assay	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575793	AUC (0 to infinity) in dog at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575808	Inhibition of human cathepsin D	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575801	Inhibition of human caspase-6 at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575807	Inhibition of bovine cathepsin C at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575785	Tmax in rat at 5 mg/kg, po	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
AID575852	Inhibition of human H3 receptor at 10 uM	2010	Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	65 (98.48)	24.3611
2020's	1 (1.52)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	29 (42.65%)	5.53%
Reviews	16 (23.53%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	23 (33.82%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
adenine [no description available]	3.48	1	1	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
carbamates [no description available]	4.4	3	0	amino-acid anion
methadone Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.	4.41	1	1	benzenes; diarylmethane; ketone; tertiary amino compound
midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.	3.5	1	1	imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative
omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.	3.51	1	1	aromatic ether; benzimidazoles; pyridines; sulfoxide
ethinyl estradiol Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.	4.41	1	1	17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound	xenoestrogen
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.	6.16	8	0	pyrimidine ribonucleoside 5'-monophosphate; uridine 5'-phosphate	Escherichia coli metabolite; human metabolite; mouse metabolite
leucine Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.	16.57	62	30	amino acid zwitterion; L-alpha-amino acid; leucine; proteinogenic amino acid; pyruvate family amino acid	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite
valine Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.	4.4	3	0	L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid; valine	algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
thiazoles [no description available]	16.57	62	30	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
levonorgestrel Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.	4.41	1	1	17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound	contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive
ethinyl estradiol-norgestrel combination Ethinyl Estradiol-Norgestrel Combination: ETHINYL ESTRADIOL and NORGESTREL given in fixed proportions.	4.41	1	1
ribavirin Rebetron: Rebetron is tradename	13.63	24	17	1-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
itraconazole Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.	2.31	1	0	aromatic ether; conazole antifungal drug; cyclic ketal; dichlorobenzene; dioxolane; N-arylpiperazine; triazole antifungal drug; triazoles	EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; Hedgehog signaling pathway inhibitor; P450 inhibitor
imiquimod Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.	3.31	1	0	imidazoquinoline	antineoplastic agent; interferon inducer
atorvastatin [no description available]	3.53	1	1	aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic)	environmental contaminant; xenobiotic
efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.	3.48	1	1	acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound	antiviral drug; HIV-1 reverse transcriptase inhibitor
norbuprenorphine norbuprenorphine: metabolite of buprenorphine found in urine & feces; RN given refers to (5alpha,7alpha)-isomer; structure given in first source	4.41	1	1	phenanthrenes
proline Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.	16.57	62	30	amino acid zwitterion; glutamine family amino acid; L-alpha-amino acid; proline; proteinogenic amino acid	algal metabolite; compatible osmolytes; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
organophosphonates hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.	3.48	1	1	divalent inorganic anion; phosphite ion
darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.	3.48	1	1	carbamate ester; furofuran; sulfonamide	antiviral drug; HIV protease inhibitor
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	3.48	1	1	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.	3.56	1	1	macrolide lactam	bacterial metabolite; immunosuppressive agent
tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.	3.48	1	1	nucleoside analogue; phosphonic acids	antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor
buprenorphine Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.	4.41	1	1	morphinane alkaloid	delta-opioid receptor antagonist; kappa-opioid receptor antagonist; mu-opioid receptor agonist; opioid analgesic
telaprevir [no description available]	5.67	7	0	cyclopentapyrrole; cyclopropanes; oligopeptide; pyrazines	antiviral drug; hepatitis C protease inhibitor; peptidomimetic
bilirubin [no description available]	5.37	2	2	biladienes; dicarboxylic acid	antioxidant; human metabolite; mouse metabolite
biln 2061 BILN 2061: a macrocyclic NS3 protease inhibitor and antiviral agent; structure in first source	4.11	4	0
n-desmethylrosuvastatin N-desmethyl rosuvastatin: a rosuvastatin metabolite	3.53	1	1	pyrimidines
sm360320 SM360320: Proc Natl Acad Sci U S A 2006 Feb 7;103(6):1828-33	3.31	1	0
n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide boceprevir : A synthetic tripeptide consisting of N-(tert-butylcarbamoyl)-3-methyl-L-valyl, a cyclopropyl-fused prolyl and 3-amino-4-cyclobutyl-2-oxobutanamide residues joined in sequence. Used for treatment of chronic hepatitis C virus genotype 1 infection.	2.48	2	0	tripeptide; ureas	antiviral drug; hepatitis C protease inhibitor; peptidomimetic
buprenorphine, naloxone drug combination Buprenorphine, Naloxone Drug Combination: A pharmaceutical preparation that combines buprenorphine, an OPIOID ANALGESICS with naloxone, a NARCOTIC ANTAGONISTS to reduce the potential for NARCOTIC DEPENDENCE in the treatment of pain. It may also be used for OPIOID SUBSTITUTION THERAPY.	4.41	1	1
danoprevir [no description available]	3.71	2	0
narlaprevir narlaprevir: an antiviral agent that inhibits hepatitis C virus NS3 protease. narlaprevir : An azabicyclohexane that is (1R,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane substituted by [(3S)-1-(cyclopropylamino)-1,2-dioxoheptan-3-yl]aminoacyl and N-({1-[(tert-butylsulfonyl)methyl]cyclohexyl}carbamoyl)-3-methyl-L-valyl groups at positions 2S and 3, respectively. It is a hepatitis C virus (HCV) NS3/4A serine protease inhibitor (Ki = 6 nM) that is used for the treatment of chronic hepatitis C.	3.31	1	0	azabicyclohexane; cyclopropanes; pyrrolidinecarboxamide; secondary carboxamide; sulfone; tertiary carboxamide; ureas	anticoronaviral agent; antiviral drug; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; hepatitis C protease inhibitor
bms-650032 asunaprevir: an NS3 protease inhibitor against hepatitis C virus	4.46	3	0	oligopeptide
raltegravir potassium Raltegravir Potassium: A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.	3.5	1	1
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.	4.65	4	0	azamacrocycle; carbamate ester; cyclopropanes; N-sulfonylcarboxamide; pyrrolidinecarboxamide	antiviral drug; hepatitis C protease inhibitor
simeprevir [no description available]	2.54	2	0	azamacrocycle; lactam
bms-790052 daclatasvir: an HCV NS5A inhibitor. daclatasvir : A member of the class of biphenyls that is a potent inhibitor of nonstructural protein 5A and is used (as its hydrochloride salt) for treatment of hepatitis C.	4.4	3	0	biphenyls; carbamate ester; carboxamide; imidazoles; valine derivative	antiviral drug; nonstructural protein 5A inhibitor
gs-9451 [no description available]	2.21	1	0
tmc647055 [no description available]	3.31	1	0
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.	3.71	2	0	aromatic 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.	2.21	1	0
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.	6.16	8	0	isopropyl ester; L-alanyl ester; nucleotide conjugate; organofluorine compound; phosphoramidate ester	antiviral drug; hepatitis C protease inhibitor; prodrug
warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.	3.5	1	1	benzenes; hydroxycoumarin; methyl ketone
deleobuvir deleobuvir: a hepatitis C virus polymerase inhibitor	14.07	9	8
cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).	3.56	1	1
danoprevir [no description available]	4.38	3	0

Condition	Indicated	Relationship Strength	Studies	Trials
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted [description not available]	0	12.39	20	8
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.	1	19.39	20	8
Chronic Hepatitis C [description not available]	0	13.5	27	17
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.	1	15.5	27	17
Co-infection [description not available]	0	6.1	4	1
HIV Coinfection [description not available]	0	10.14	9	5
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).	1	12.14	9	5
HIV Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.	0	8.01	1	0
Cirrhosis, Liver [description not available]	0	7.05	3	2
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.	0	7.05	3	2
Bilirubinemia [description not available]	0	3.48	1	1
Kidney Failure A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.	0	4.41	1	1
Renal Insufficiency Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.	1	6.41	1	1
Chemical Dependence [description not available]	0	4.41	1	1
Drug Withdrawal Symptoms [description not available]	0	4.41	1	1
Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.	0	4.41	1	1
Substance-Related Disorders Disorders related to substance use or abuse.	0	4.41	1	1
Viremia The presence of viruses in the blood.	0	7.54	4	4
Anemia A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.	0	4.41	1	1

bi 201335

Description

Cross-References

Synonyms (28)

Research Excerpts

Overview

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Protein Targets (7)

Inhibition Measurements

Biological Processes (66)

Molecular Functions (20)

Ceullar Components (27)

Bioassays (153)

Research

Studies (66)

Market Indicators

Research Demand Index: 17.28

Study Types

bi 201335

Description

Cross-References

Synonyms (28)

Research Excerpts

Overview

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Protein Targets (7)

Inhibition Measurements

Biological Processes (66)

Molecular Functions (20)

Ceullar Components (27)

Bioassays (153)

Research

Studies (66)

Market Indicators

Research Demand Index: 17.28

Study Types

Related Drugs (48)

Related Conditions (19)