mk-7009 profile

vaniprevir: inhibits hepatitis C virus NS3/4a protease [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	24765256
CHEMBL ID	4525964
SCHEMBL ID	3264200
MeSH ID	M0535390

Synonym
HY-10243
vaniprevir
mk-7009
923590-37-8
unii-cv3x74ao1h
cv3x74ao1h ,
mk 7009
mk7009
vanihep
vaniprevir [usan:inn]
cyclopropanecarboxamide, n-(((6-(2-carboxy-2,3-dihydro-1h-isoindol-4-yl)-2,2-dimethylhexyl)oxy)carbonyl)-3-methyl-l-valyl-(4r)-4-hydroxy-l-prolyl-1-amino-n-(cyclopropylsulfonyl)-2-ethyl-, (1-2)-lactone, (1r,2r)-
bdbm103836
CS-0340
3SU6
vaniprevir [who-dd]
vaniprevir [inn]
cyclopropanecarboxamide, n-(((6-(2-carboxy-2,3-dihydro-1h-isoindol-4-yl)-2,2-dimethylhexyl)oxy)carbonyl)-3-methyl-l-valyl-(4r)-4-hydroxy-l-prolyl-1-amino-n-(cyclopropylsulfonyl)-2-ethyl-, (1->2)-lactone, (1r,2r)-
vaniprevir [jan]
vaniprevir [mi]
vaniprevir [usan]
SCHEMBL3264200
AKOS030527003
CHEMBL4525964
NCGC00485973-01
DB11929
vaniprevir; mk-7009
(1r,21s,24s)-21-tert-butyl-n-[(1r,2r)-1-(cyclopropylsulfonylcarbamoyl)-2-ethylcyclopropyl]-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6(11),7,9-triene-24-carboxamide
mk-7009;mk 7009;vaniprevir
BCP09841
Q7914945
gtpl11570
DTXSID201029738

Excerpt	Reference	Relevance
" The most commonly reported drug-related adverse events (AEs) were diarrhea (n=5) and nausea (n=5)."	( Characterization of vaniprevir, a hepatitis C virus NS3/4A protease inhibitor, in patients with HCV genotype 1 infection: safety, antiviral activity, resistance, and pharmacokinetics. Al-Ibrahim, M; Barnard, R; Caro, L; Gordon, SC; Gress, J; Hwang, PM; Jacobson, I; Kraft, WK; Kwo, P; Lawitz, E; Maliakkal, B; Miller, M; Mobashery, N; Panorchan, P; Quirk, E; Rockstroh, JK; Sulkowski, M, 2013)	0.39

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Role	Description
hepatitis C protease inhibitor	An inhibitor of hepatitis C protease, an enzyme required for production of proteins needed for viral assembly.
antiviral drug	A substance used in the prophylaxis or therapy of virus diseases.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
azamacrocycle	A cyclic macromolecule containing one or more nitrogen atoms in place of carbon either as the divalent group NH for the group CH2 or a single trivalent nitrogen atom for the group CH.
N-sulfonylcarboxamide	A mixed diacylamine resulting from the formal condensation of the nitrogen of a carboxamide with a sulphonic acid.
cyclopropanes	Cyclopropane and its derivatives formed by substitution.
pyrrolidinecarboxamide
carbamate ester	Any ester of carbamic acid or its N-substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Genome polyprotein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, Genome polyprotein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, Genome polyprotein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease,NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Chain A, NS3 protease, NS4A protein		Ki	0.9580	0.9580	0.9580	0.9580	AID977610
Genome polyprotein		Ki	0.0095	0.0000	0.0067	0.0300	AID1173945; AID673711
Non-structural protein 4A		Ki	0.0095	0.0000	0.0067	0.0300	AID1173945; AID673711
Genome polyprotein		Ki	0.0623	0.0001	0.0341	0.0880	AID673712; AID673713; AID673714
Cathepsin L2	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0750	2.2141	10.0000	AID508158
Prothrombin	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0000	0.7107	10.0000	AID781217
Plasminogen	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0250	3.6280	10.0000	AID781219
Trypsin-1	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0035	1.5321	10.0000	AID508175
Procathepsin L	Homo sapiens (human)	IC50 (µMol)	10,000.0000	0.0002	1.6661	9.5100	AID508157
Cathepsin B	Homo sapiens (human)	IC50 (µMol)	10,000.0000	0.0002	1.8453	10.0000	AID508174
Neutrophil elastase	Homo sapiens (human)	IC50 (µMol)	55.0000	0.0063	2.0734	22.3780	AID508161; AID781220
Chymase	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0260	2.6397	10.0000	AID508159
Cathepsin S	Homo sapiens (human)	IC50 (µMol)	44.0000	0.0002	1.3191	10.0000	AID508156; AID781218
Genome polyprotein	Hepatitis C virus (isolate H77)	Ki	0.0005	0.0005	0.0095	0.0140	AID1800083
Cathepsin K	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0001	0.8482	10.0000	AID508172
Cathepsin F	Homo sapiens (human)	IC50 (µMol)	10.0000	0.7950	0.9475	1.1000	AID508173
Chymotrypsin-like elastase family member 1	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0300	0.0408	0.0516	AID508160
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Prothrombin	Homo sapiens (human)	IC90 (µMol)	100.0000	1.0000	1.2000	1.4000	AID781217
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
apoptotic process	Cathepsin L2	Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class II	Cathepsin L2	Homo sapiens (human)
extracellular matrix disassembly	Cathepsin L2	Homo sapiens (human)
immune response	Cathepsin L2	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Cathepsin L2	Homo sapiens (human)
positive regulation of peptidase activity	Cathepsin L2	Homo sapiens (human)
proteolysis involved in protein catabolic process	Cathepsin L2	Homo sapiens (human)
positive regulation of protein phosphorylation	Prothrombin	Homo sapiens (human)
proteolysis	Prothrombin	Homo sapiens (human)
acute-phase response	Prothrombin	Homo sapiens (human)
cell surface receptor signaling pathway	Prothrombin	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Prothrombin	Homo sapiens (human)
blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of cell population proliferation	Prothrombin	Homo sapiens (human)
regulation of cell shape	Prothrombin	Homo sapiens (human)
response to wounding	Prothrombin	Homo sapiens (human)
negative regulation of platelet activation	Prothrombin	Homo sapiens (human)
platelet activation	Prothrombin	Homo sapiens (human)
regulation of blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of blood coagulation	Prothrombin	Homo sapiens (human)
positive regulation of cell growth	Prothrombin	Homo sapiens (human)
positive regulation of insulin secretion	Prothrombin	Homo sapiens (human)
positive regulation of collagen biosynthetic process	Prothrombin	Homo sapiens (human)
fibrinolysis	Prothrombin	Homo sapiens (human)
negative regulation of proteolysis	Prothrombin	Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STAT	Prothrombin	Homo sapiens (human)
negative regulation of astrocyte differentiation	Prothrombin	Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol	Prothrombin	Homo sapiens (human)
regulation of cytosolic calcium ion concentration	Prothrombin	Homo sapiens (human)
cytolysis by host of symbiont cells	Prothrombin	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Prothrombin	Homo sapiens (human)
negative regulation of fibrinolysis	Prothrombin	Homo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptide	Prothrombin	Homo sapiens (human)
neutrophil-mediated killing of gram-negative bacterium	Prothrombin	Homo sapiens (human)
positive regulation of lipid kinase activity	Prothrombin	Homo sapiens (human)
negative regulation of cytokine production involved in inflammatory response	Prothrombin	Homo sapiens (human)
positive regulation of protein localization to nucleus	Prothrombin	Homo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathway	Prothrombin	Homo sapiens (human)
ligand-gated ion channel signaling pathway	Prothrombin	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Prothrombin	Homo sapiens (human)
proteolysis	Plasminogen	Homo sapiens (human)
blood coagulation	Plasminogen	Homo sapiens (human)
negative regulation of cell population proliferation	Plasminogen	Homo sapiens (human)
negative regulation of cell-substrate adhesion	Plasminogen	Homo sapiens (human)
extracellular matrix disassembly	Plasminogen	Homo sapiens (human)
tissue regeneration	Plasminogen	Homo sapiens (human)
fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Plasminogen	Homo sapiens (human)
myoblast differentiation	Plasminogen	Homo sapiens (human)
muscle cell cellular homeostasis	Plasminogen	Homo sapiens (human)
tissue remodeling	Plasminogen	Homo sapiens (human)
biological process involved in interaction with symbiont	Plasminogen	Homo sapiens (human)
negative regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
trophoblast giant cell differentiation	Plasminogen	Homo sapiens (human)
labyrinthine layer blood vessel development	Plasminogen	Homo sapiens (human)
mononuclear cell migration	Plasminogen	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Plasminogen	Homo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherin	Plasminogen	Homo sapiens (human)
digestion	Trypsin-1	Homo sapiens (human)
extracellular matrix disassembly	Trypsin-1	Homo sapiens (human)
proteolysis	Trypsin-1	Homo sapiens (human)
adaptive immune response	Procathepsin L	Homo sapiens (human)
proteolysis	Procathepsin L	Homo sapiens (human)
protein autoprocessing	Procathepsin L	Homo sapiens (human)
fusion of virus membrane with host plasma membrane	Procathepsin L	Homo sapiens (human)
receptor-mediated endocytosis of virus by host cell	Procathepsin L	Homo sapiens (human)
antigen processing and presentation	Procathepsin L	Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class II	Procathepsin L	Homo sapiens (human)
collagen catabolic process	Procathepsin L	Homo sapiens (human)
zymogen activation	Procathepsin L	Homo sapiens (human)
enkephalin processing	Procathepsin L	Homo sapiens (human)
fusion of virus membrane with host endosome membrane	Procathepsin L	Homo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitment	Procathepsin L	Homo sapiens (human)
symbiont entry into host cell	Procathepsin L	Homo sapiens (human)
antigen processing and presentation of peptide antigen	Procathepsin L	Homo sapiens (human)
proteolysis involved in protein catabolic process	Procathepsin L	Homo sapiens (human)
elastin catabolic process	Procathepsin L	Homo sapiens (human)
macrophage apoptotic process	Procathepsin L	Homo sapiens (human)
cellular response to thyroid hormone stimulus	Procathepsin L	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Procathepsin L	Homo sapiens (human)
positive regulation of peptidase activity	Procathepsin L	Homo sapiens (human)
immune response	Procathepsin L	Homo sapiens (human)
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)
angiotensin maturation	Chymase	Homo sapiens (human)
peptide metabolic process	Chymase	Homo sapiens (human)
extracellular matrix disassembly	Chymase	Homo sapiens (human)
protein catabolic process	Chymase	Homo sapiens (human)
midbrain development	Chymase	Homo sapiens (human)
basement membrane disassembly	Chymase	Homo sapiens (human)
positive regulation of angiogenesis	Chymase	Homo sapiens (human)
regulation of inflammatory response	Chymase	Homo sapiens (human)
cellular response to glucose stimulus	Chymase	Homo sapiens (human)
cytokine precursor processing	Chymase	Homo sapiens (human)
toll-like receptor signaling pathway	Cathepsin S	Homo sapiens (human)
adaptive immune response	Cathepsin S	Homo sapiens (human)
proteolysis	Cathepsin S	Homo sapiens (human)
apoptotic process	Cathepsin S	Homo sapiens (human)
response to acidic pH	Cathepsin S	Homo sapiens (human)
protein processing	Cathepsin S	Homo sapiens (human)
antigen processing and presentation	Cathepsin S	Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class II	Cathepsin S	Homo sapiens (human)
extracellular matrix disassembly	Cathepsin S	Homo sapiens (human)
collagen catabolic process	Cathepsin S	Homo sapiens (human)
basement membrane disassembly	Cathepsin S	Homo sapiens (human)
antigen processing and presentation of peptide antigen	Cathepsin S	Homo sapiens (human)
proteolysis involved in protein catabolic process	Cathepsin S	Homo sapiens (human)
cellular response to thyroid hormone stimulus	Cathepsin S	Homo sapiens (human)
positive regulation of cation channel activity	Cathepsin S	Homo sapiens (human)
positive regulation of peptidase activity	Cathepsin S	Homo sapiens (human)
immune response	Cathepsin S	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Cathepsin S	Homo sapiens (human)
collagen catabolic process	Cathepsin K	Homo sapiens (human)
mitophagy	Cathepsin K	Homo sapiens (human)
intramembranous ossification	Cathepsin K	Homo sapiens (human)
proteolysis	Cathepsin K	Homo sapiens (human)
thyroid hormone generation	Cathepsin K	Homo sapiens (human)
apoptotic process	Cathepsin K	Homo sapiens (human)
response to organic cyclic compound	Cathepsin K	Homo sapiens (human)
extracellular matrix disassembly	Cathepsin K	Homo sapiens (human)
collagen catabolic process	Cathepsin K	Homo sapiens (human)
response to insulin	Cathepsin K	Homo sapiens (human)
cellular response to zinc ion starvation	Cathepsin K	Homo sapiens (human)
bone resorption	Cathepsin K	Homo sapiens (human)
response to ethanol	Cathepsin K	Homo sapiens (human)
proteolysis involved in protein catabolic process	Cathepsin K	Homo sapiens (human)
negative regulation of cartilage development	Cathepsin K	Homo sapiens (human)
cellular response to tumor necrosis factor	Cathepsin K	Homo sapiens (human)
cellular response to transforming growth factor beta stimulus	Cathepsin K	Homo sapiens (human)
mononuclear cell differentiation	Cathepsin K	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Cathepsin K	Homo sapiens (human)
positive regulation of peptidase activity	Cathepsin K	Homo sapiens (human)
immune response	Cathepsin K	Homo sapiens (human)
proteolysis	Cathepsin F	Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class II	Cathepsin F	Homo sapiens (human)
proteolysis involved in protein catabolic process	Cathepsin F	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
transcription by RNA polymerase II	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
inflammatory response	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
post-embryonic development	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
Wnt signaling pathway	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
exocrine pancreas development	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
multicellular organism growth	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
regulation of cell population proliferation	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
regulation of cell differentiation	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
positive regulation of angiogenesis	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
tissue remodeling	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
elastin catabolic process	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
pancreas morphogenesis	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
proteolysis	Chymotrypsin-like elastase family member 1	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 L2	Homo sapiens (human)
serine-type endopeptidase activity	Cathepsin L2	Homo sapiens (human)
protein binding	Cathepsin L2	Homo sapiens (human)
cysteine-type peptidase activity	Cathepsin L2	Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic process	Cathepsin L2	Homo sapiens (human)
lipopolysaccharide binding	Prothrombin	Homo sapiens (human)
serine-type endopeptidase activity	Prothrombin	Homo sapiens (human)
signaling receptor binding	Prothrombin	Homo sapiens (human)
calcium ion binding	Prothrombin	Homo sapiens (human)
protein binding	Prothrombin	Homo sapiens (human)
growth factor activity	Prothrombin	Homo sapiens (human)
heparin binding	Prothrombin	Homo sapiens (human)
thrombospondin receptor activity	Prothrombin	Homo sapiens (human)
protease binding	Plasminogen	Homo sapiens (human)
endopeptidase activity	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Plasminogen	Homo sapiens (human)
signaling receptor binding	Plasminogen	Homo sapiens (human)
protein binding	Plasminogen	Homo sapiens (human)
serine-type peptidase activity	Plasminogen	Homo sapiens (human)
enzyme binding	Plasminogen	Homo sapiens (human)
kinase binding	Plasminogen	Homo sapiens (human)
protein domain specific binding	Plasminogen	Homo sapiens (human)
apolipoprotein binding	Plasminogen	Homo sapiens (human)
protein-folding chaperone binding	Plasminogen	Homo sapiens (human)
protein antigen binding	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Trypsin-1	Homo sapiens (human)
metal ion binding	Trypsin-1	Homo sapiens (human)
fibronectin binding	Procathepsin L	Homo sapiens (human)
cysteine-type endopeptidase activity	Procathepsin L	Homo sapiens (human)
protein binding	Procathepsin L	Homo sapiens (human)
collagen binding	Procathepsin L	Homo sapiens (human)
cysteine-type peptidase activity	Procathepsin L	Homo sapiens (human)
histone binding	Procathepsin L	Homo sapiens (human)
proteoglycan binding	Procathepsin L	Homo sapiens (human)
serpin family protein binding	Procathepsin L	Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic process	Procathepsin L	Homo sapiens (human)
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)
endopeptidase activity	Chymase	Homo sapiens (human)
serine-type endopeptidase activity	Chymase	Homo sapiens (human)
serine-type peptidase activity	Chymase	Homo sapiens (human)
peptide binding	Chymase	Homo sapiens (human)
fibronectin binding	Cathepsin S	Homo sapiens (human)
cysteine-type endopeptidase activity	Cathepsin S	Homo sapiens (human)
serine-type endopeptidase activity	Cathepsin S	Homo sapiens (human)
collagen binding	Cathepsin S	Homo sapiens (human)
laminin binding	Cathepsin S	Homo sapiens (human)
proteoglycan binding	Cathepsin S	Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic process	Cathepsin S	Homo sapiens (human)
fibronectin binding	Cathepsin K	Homo sapiens (human)
cysteine-type endopeptidase activity	Cathepsin K	Homo sapiens (human)
serine-type endopeptidase activity	Cathepsin K	Homo sapiens (human)
protein binding	Cathepsin K	Homo sapiens (human)
collagen binding	Cathepsin K	Homo sapiens (human)
cysteine-type peptidase activity	Cathepsin K	Homo sapiens (human)
proteoglycan binding	Cathepsin K	Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic process	Cathepsin K	Homo sapiens (human)
cysteine-type endopeptidase activity	Cathepsin F	Homo sapiens (human)
serine-type endopeptidase activity	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
metal ion binding	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular region	Cathepsin L2	Homo sapiens (human)
lysosomal lumen	Cathepsin L2	Homo sapiens (human)
extracellular space	Cathepsin L2	Homo sapiens (human)
lysosome	Cathepsin L2	Homo sapiens (human)
external side of plasma membrane	Prothrombin	Homo sapiens (human)
collagen-containing extracellular matrix	Prothrombin	Homo sapiens (human)
extracellular region	Prothrombin	Homo sapiens (human)
extracellular space	Prothrombin	Homo sapiens (human)
endoplasmic reticulum lumen	Prothrombin	Homo sapiens (human)
Golgi lumen	Prothrombin	Homo sapiens (human)
plasma membrane	Prothrombin	Homo sapiens (human)
extracellular exosome	Prothrombin	Homo sapiens (human)
blood microparticle	Prothrombin	Homo sapiens (human)
collagen-containing extracellular matrix	Prothrombin	Homo sapiens (human)
extracellular space	Prothrombin	Homo sapiens (human)
extracellular region	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
plasma membrane	Plasminogen	Homo sapiens (human)
external side of plasma membrane	Plasminogen	Homo sapiens (human)
cell surface	Plasminogen	Homo sapiens (human)
platelet alpha granule lumen	Plasminogen	Homo sapiens (human)
collagen-containing extracellular matrix	Plasminogen	Homo sapiens (human)
extracellular exosome	Plasminogen	Homo sapiens (human)
blood microparticle	Plasminogen	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Plasminogen	Homo sapiens (human)
glutamatergic synapse	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
extracellular region	Trypsin-1	Homo sapiens (human)
collagen-containing extracellular matrix	Trypsin-1	Homo sapiens (human)
blood microparticle	Trypsin-1	Homo sapiens (human)
extracellular space	Trypsin-1	Homo sapiens (human)
extracellular region	Procathepsin L	Homo sapiens (human)
extracellular space	Procathepsin L	Homo sapiens (human)
nucleus	Procathepsin L	Homo sapiens (human)
lysosome	Procathepsin L	Homo sapiens (human)
multivesicular body	Procathepsin L	Homo sapiens (human)
Golgi apparatus	Procathepsin L	Homo sapiens (human)
plasma membrane	Procathepsin L	Homo sapiens (human)
apical plasma membrane	Procathepsin L	Homo sapiens (human)
endolysosome lumen	Procathepsin L	Homo sapiens (human)
chromaffin granule	Procathepsin L	Homo sapiens (human)
lysosomal lumen	Procathepsin L	Homo sapiens (human)
intracellular membrane-bounded organelle	Procathepsin L	Homo sapiens (human)
collagen-containing extracellular matrix	Procathepsin L	Homo sapiens (human)
extracellular exosome	Procathepsin L	Homo sapiens (human)
endocytic vesicle lumen	Procathepsin L	Homo sapiens (human)
extracellular space	Procathepsin L	Homo sapiens (human)
lysosome	Procathepsin L	Homo sapiens (human)
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)
collagen-containing extracellular matrix	Chymase	Homo sapiens (human)
extracellular region	Chymase	Homo sapiens (human)
cytosol	Chymase	Homo sapiens (human)
secretory granule	Chymase	Homo sapiens (human)
cytoplasmic ribonucleoprotein granule	Chymase	Homo sapiens (human)
collagen-containing extracellular matrix	Chymase	Homo sapiens (human)
extracellular space	Chymase	Homo sapiens (human)
intracellular membrane-bounded organelle	Chymase	Homo sapiens (human)
cytoplasm	Chymase	Homo sapiens (human)
extracellular region	Cathepsin S	Homo sapiens (human)
extracellular space	Cathepsin S	Homo sapiens (human)
lysosome	Cathepsin S	Homo sapiens (human)
late endosome	Cathepsin S	Homo sapiens (human)
endolysosome lumen	Cathepsin S	Homo sapiens (human)
lysosomal lumen	Cathepsin S	Homo sapiens (human)
intracellular membrane-bounded organelle	Cathepsin S	Homo sapiens (human)
phagocytic vesicle	Cathepsin S	Homo sapiens (human)
collagen-containing extracellular matrix	Cathepsin S	Homo sapiens (human)
tertiary granule lumen	Cathepsin S	Homo sapiens (human)
ficolin-1-rich granule lumen	Cathepsin S	Homo sapiens (human)
extracellular space	Cathepsin S	Homo sapiens (human)
lysosome	Cathepsin S	Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membrane	Genome polyprotein	Hepatitis C virus (isolate H77)
extracellular region	Cathepsin K	Homo sapiens (human)
extracellular space	Cathepsin K	Homo sapiens (human)
nucleoplasm	Cathepsin K	Homo sapiens (human)
lysosome	Cathepsin K	Homo sapiens (human)
external side of plasma membrane	Cathepsin K	Homo sapiens (human)
apical plasma membrane	Cathepsin K	Homo sapiens (human)
endolysosome lumen	Cathepsin K	Homo sapiens (human)
lysosomal lumen	Cathepsin K	Homo sapiens (human)
intracellular membrane-bounded organelle	Cathepsin K	Homo sapiens (human)
extracellular space	Cathepsin K	Homo sapiens (human)
lysosome	Cathepsin K	Homo sapiens (human)
lysosome	Cathepsin F	Homo sapiens (human)
endoplasmic reticulum	Cathepsin F	Homo sapiens (human)
plasma membrane	Cathepsin F	Homo sapiens (human)
lysosomal lumen	Cathepsin F	Homo sapiens (human)
intracellular membrane-bounded organelle	Cathepsin F	Homo sapiens (human)
collagen-containing extracellular matrix	Cathepsin F	Homo sapiens (human)
extracellular exosome	Cathepsin F	Homo sapiens (human)
extracellular vesicle	Cathepsin F	Homo sapiens (human)
lysosome	Cathepsin F	Homo sapiens (human)
extracellular space	Cathepsin F	Homo sapiens (human)
extracellular space	Chymotrypsin-like elastase family member 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (159)

Assay ID	Title	Year	Journal	Article
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID460006	Cmax in monkey at 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508161	Inhibition of human Neutrophil elastase 2	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508208	Half life in rhesus monkey at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID491860	Inhibition of HCV NS3 protease by FRET assay	2010	Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14	Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents.
AID459989	Antiviral activity against HCV JFH-1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 10% fetal bovine serum	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508216	Antiviral activity against Hepatitis C virus containing NS3/4a ps36 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781220	Inhibition of human neutrophil elastase	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID781235	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease R155K mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508163	Inhibition of human CYP2D6	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID516850	Antiviral activity against HCV 1a infected in human hepatoma cells by replicon assay	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates.
AID508193	Metabolic stability in rhesus monkey liver assessed as drug level at 5 mg/kg, po after 24 hrs by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508197	AUC (0-24 hrs) in rhesus monkey at 5 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508218	Antiviral activity against Hepatitis C virus containing NS3/4a ps38 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID673709	Inhibition of Hepatitis C virus (isolate NZL1) genotype 3a NS3/4a protease expressed in Escherichia coli by time-resolved fluorescence analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID508171	Antiviral activity against Hepatitis C virus containing NS3/4a ps33 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508196	AUC (0-24 hrs) in chimpanzee at 10 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A 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
AID781232	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease D168V mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508175	Inhibition of human Trypsin activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781231	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease V36M mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508164	Inhibition of human CYP2C9	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781241	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease A156T mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID781219	Inhibition of human plasmin	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508181	Antiviral activity against Hepatitis C virus containing NS3/Q41R protease mutant activity by TaqMan-based assay	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781217	Inhibition of human thrombin	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID460007	AUC in monkey at 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID781221	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease D168A mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID673711	Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease R155K mutant expressed in Escherichia coli by time-resolved fluorescence analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID781239	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease A156T mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508194	Metabolic stability in dog liver assessed as drug level at 5 mg/kg, po after 24 hrs by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID664164	Antiviral activity against Hepatitis C virus subtype 1b harboring protease A156T mutant by transient replicon assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.
AID673722	Antiviral activity against Hepatitis C virus (isolate Con1) genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% NHS	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID460012	Ratio of drug level in Sprague-Dawley rat liver after 24 hrs to IC50 for HCV Con1 infected in human HuH7 cells in presence of 10% fetal bovine serum	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508199	AUC (0-24 hrs) in rat at 5 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508182	Antiviral activity against Hepatitis C virus genotype 1a containing NS3/con1 protease mutant by TaqMan-based assay	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508160	Inhibition of human Pancreatic elastase 1	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781224	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease V170A mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508215	Plasma clearance in dog at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460002	Drug level in Beagle dog liver at 5 mg/kg, po after 24 hrs by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID459993	Cmax in Sprague-Dawley rat at 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID781236	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease D168A mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID459996	Clearance in Beagle dog at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508159	Inhibition of human Chymase	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460004	Volume of distribution in monkey at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508209	Half life in rat at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508195	Metabolic stability in rat liver assessed as drug level at 5 mg/kg, po after 24 hrs by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508169	Antiviral activity against Hepatitis C virus containing NS3/4a ps31 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508192	Metabolic stability in chimpanzee liver assessed as drug level at 10 mg/kg, po after 12 hrs by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781228	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease A156S mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID781229	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease V36M mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508187	Inhibition of Hepatitis C virus genotype 2b NS3/4A protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460011	Drug level in chimpanzee liver at 10 mg/kg, po after 12 hrs by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID781240	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease A156T mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID459987	Antiviral activity against HCV Con1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 50% normal human serum	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID460010	AUC in chimpanzee at 10 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508190	Inhibition of Hepatitis C virus genotype 1a NS3/4A protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508172	Inhibition of human Cathepsin K	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459999	Cmax in Beagle dog at 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID459985	Inhibition of HCV JFH-1 full length NS3/4A protease expressed in Escherichia coli after 1 hr by time-resolved fluorescence assay	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
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.
AID781233	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease D168V mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID584105	Antiviral activity against HCV1b harboring Q80Q polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID673708	Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease expressed in Escherichia coli by time-resolved fluorescence analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID508213	Plasma clearance in rhesus monkey at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID673712	Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease A156T mutant expressed in Escherichia coli by time-resolved fluorescence analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID781218	Inhibition of human cathepsin S	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508212	Volume of distribution in rat at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459991	Volume of distribution in Sprague-Dawley rat at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID781238	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease R155K mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508188	Inhibition of Hepatitis C virus genotype 2a NS3/4A protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459998	Half life in Beagle dog at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508177	Antiviral activity against Hepatitis C virus containing NS3/D168Y protease mutant activity by TaqMan-based assay	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459990	Clearance in Sprague-Dawley rat at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508189	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781227	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease A156S mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID781234	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease D168V mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508206	AUC (0-24 hrs) in rat at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781226	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease A156S mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508158	Inhibition of human Cathepsin V	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508176	Inhibition of human Chymotrypsin	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508186	Antiviral activity against Hepatitis C virus genotype 1b infected in mouse HB1 cell by cell-based HCV replicon assay in presence of 10% fetal bovine serum	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508162	Inhibition of human CYP3A4	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460014	Ratio of drug level in chimpanzee liver after 12 hrs to IC50 for HCV Con1 infected in human HuH7 cells in presence of 50% normal human serum	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID673714	Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease D168V mutant expressed in Escherichia coli by time-resolved fluorescence analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID508198	AUC (0-24 hrs) in dog at 5 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508200	Cmax in Chimpanzee at 10 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID491861	Antiviral activity against HCV 1B infected in human Huh7 cells by firefly luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14	Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents.
AID508184	Antiviral activity against Hepatitis C virus genotype 2a infected in mouse HB1 cell by cell-based HCV replicon assay in presence of 10% fetal bovine serum	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508219	Antiviral activity against Hepatitis C virus containing NS3/4a ps40 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508207	Half life in dog at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508170	Antiviral activity against Hepatitis C virus containing NS3/4a ps32 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508191	Plasma clearance in chimpanzee at 10 mg/kg, po after 12 hrs by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508173	Inhibition of human Cathepsin F	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781230	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease V36M mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID781242	Inhibition of Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508217	Antiviral activity against Hepatitis C virus containing NS3/4a ps37 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID715382	Inhibition of HCV3a NS3/4A protease	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
AID584107	Ratio of EC50 for HCV1b harboring Q80K polymorphism in NS3 protease gene to EC50 for HCV1b harboring Q80Q polymorphism in NS3 protease gene	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID460008	Drug level in monkey liver at 5 mg/kg, po after 2 hrs by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID673710	Drug uptake in Sprague-Dawley rat liver at 5 mg/kg, po after 4 hrs by HPLC analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID781222	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease D168A mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID459997	Volume of distribution in Beagle dog at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508156	Inhibition of human Cathepsin S	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508167	Antiviral activity against Hepatitis C virus containing NS3/4a ps20 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508214	Plasma clearance in rat at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459984	Inhibition of HCV1b BK full length NS3/4A protease expressed in Escherichia coli after 1 hr by time-resolved fluorescence assay	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508174	Inhibition of human Cathepsin B	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460000	AUC in Beagle dog at 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID1645924	Antiviral activity against HCV	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	A review on HCV inhibitors: Significance of non-structural polyproteins.
AID673713	Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease A156V mutant expressed in Escherichia coli by time-resolved fluorescence analysis	2012	ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4	Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
AID508205	AUC (0-24 hrs) in dog at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508168	Antiviral activity against Hepatitis C virus containing NS3/4a ps30 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781225	Inhibition of Hepatitis C virus genotype 1b NS3/4A protease V170A mutant	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508210	Volume of distribution in rhesus monkey at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A 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.
AID508220	Antiviral activity against Hepatitis C virus containing NS3/4a ps41 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID584102	Antiviral activity against HCV1b Con1 harboring NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID459992	Half life in Sprague-Dawley rat at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508157	Inhibition of human Cathepsin L	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460003	Clearance in monkey at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID584109	Ratio of EC50 for wild type HCV1b harboring NS3 protease gene to EC50 for HCV1b harboring NS3 protease Q80K mutant	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID508185	Antiviral activity against Hepatitis C virus genotype 1b infected in mouse HB1 cell by cell-based HCV replicon assay in presence of 50% normal human serum	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459986	Antiviral activity against HCV Con1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 10% fetal bovine serum	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508178	Antiviral activity against Hepatitis C virus containing NS3/A156T protease mutant activity by TaqMan-based assay	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459988	Drug level in Sprague-Dawley rat liver at 5 mg/kg, po after 4 hrs by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID664166	Antiviral activity against wild type Hepatitis C virus subtype 1b by transient replicon assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.
AID459994	AUC in Sprague-Dawley rat at 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID584106	Antiviral activity against HCV1b harboring Q80K polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID508166	Antiviral activity against Hepatitis C virus containing NS3/4a H77 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781223	Ratio of EC90 for Hepatitis C virus genotype 1b NS3/4A protease V170A mutant to EC90 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508165	Antiviral activity against Hepatitis C virus containing NS3/4a Con1 sequence by transient cell-base protease activity	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID781237	Ratio of EC50 for Hepatitis C virus genotype 1b NS3/4A protease R155K mutant to EC50 Hepatitis C virus genotype 1b wild type NS3/4A protease	2013	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.
AID508211	Volume of distribution in dog at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID584110	Ratio of EC50 for wild type HCV1b harboring NS3 protease gene to EC50 for HCV1b harboring NS3 protease Q80K, T54S mutant	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID508180	Antiviral activity against Hepatitis C virus containing NS3/F43S protease mutant activity by TaqMan-based assay	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID584101	Ratio of EC50 for wild type HCV1b harboring NS3 protease gene to EC50 for HCV1b B13 harboring NS3 protease R26K, V46I, Q80L mutant	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID460005	Half life in monkey at 2 mg/kg, iv and 5 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID584103	Ratio of EC50 for wild type HCV1b harboring NS3 protease gene to EC50 for HCV1b A25 harboring NS3 protease T40A, T54S, V55I, I64L, P67S, Q80K, Q88H, S90A, L153I mutant	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID508204	AUC (0-24 hrs) in rhesus monkey at 2 mg/kg, iv by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID459995	Drug level in Sprague-Dawley rat liver at 5 mg/kg, po after 24 hrs by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID664167	Antiviral activity against Hepatitis C virus subtype 1b harboring protease R155K mutant by transient replicon assay	2012	Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7	Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.
AID516851	Antiviral activity against HCV 1b infected in human hepatoma cells by replicon assay	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates.
AID508203	Cmax in rat at 5 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508202	Cmax in rhesus monkey at 5 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508201	Cmax in dog at 5 mg/kg, po by LC/MS/MS analysis	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID508183	Cytotoxicity against mouse HB-1 cells	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID460013	Ratio of drug level in Sprague-Dawley rat liver after 24 hrs to IC50 for HCV Con1 infected in human HuH7 cells in presence of 50% normal human serum	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID460001	Drug level in Beagle dog liver at 5 mg/kg, po after 2 hrs by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID584104	Ratio of EC50 for wild type HCV1b harboring NS3 protease gene to EC50 for HCV1b B10 harboring NS3 protease S7A, R26K, V48I, T54S mutant	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID460009	Cmax in chimpanzee at 10 mg/kg, po by LC/MS analysis	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
AID508179	Antiviral activity against Hepatitis C virus containing NS3/R155K protease mutant activity by TaqMan-based assay	2010	Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
AID584108	Ratio of EC50 for wild type HCV1b harboring NS3 protease gene to EC50 for HCV1b harboring NS3 protease T54S mutant	2010	Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12	Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.
AID977610	Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB	2012	PLoS pathogens, , Volume: 8, Issue:7	The molecular basis of drug resistance against hepatitis C virus NS3/4A protease inhibitors.
AID1800083	Enzyme Inhibition Assay from Article 10.1021/cb400100g: \\Evaluating the Role of Macrocycles in the Susceptibility of Hepatitis C Virus NS3/4A Protease Inhibitors to Drug Resistance.\\	2013	ACS chemical biology, Jul-19, Volume: 8, Issue:7	Evaluating the role of macrocycles in the susceptibility of hepatitis C virus NS3/4A protease inhibitors to drug resistance.
[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	1 (2.38)	29.6817
2010's	38 (90.48)	24.3611
2020's	3 (7.14)	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	12 (28.57%)	5.53%
Reviews	3 (7.14%)	6.00%
Case Studies	1 (2.38%)	4.05%
Observational	0 (0.00%)	0.25%
Other	26 (61.90%)	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
carbamates [no description available]	2.1	1	0	amino-acid anion
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.	13.44	33	16	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
tubercidin Tubercidin: An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.. tubercidin : An N-glycosylpyrrolopyrimidine that is adenosine in which the in the 5-membered ring that is not attached to the ribose moiety is replaced by a carbon. Tubercidin is produced in the culture broth of Streptomyces tubericidus.	2.06	1	0	antibiotic antifungal agent; N-glycosylpyrrolopyrimidine; ribonucleoside	antimetabolite; antineoplastic agent; bacterial metabolite
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	2.1	1	0	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
succinamide [no description available]	2.05	1	0
thiazoles [no description available]	3.16	1	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
palladium Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46.	2.06	1	0	metal allergen; nickel group element atom; platinum group metal atom
ruthenium Ruthenium: A hard, brittle, grayish-white rare earth metal with an atomic symbol Ru, atomic number 44, and atomic weight 101.07. It is used as a catalyst and hardener for PLATINUM and PALLADIUM.	2.07	1	0	iron group element atom; platinum group metal atom
ribavirin Rebetron: Rebetron is tradename	14.58	10	9	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
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
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.	13.44	33	16	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
telaprevir [no description available]	3.57	8	0	cyclopentapyrrole; cyclopropanes; oligopeptide; pyrazines	antiviral drug; hepatitis C protease inhibitor; peptidomimetic
mk 0608 7-deaza-2'-C-methyladenosine: an antiviral agent	2.06	1	0
biln 2061 BILN 2061: a macrocyclic NS3 protease inhibitor and antiviral agent; structure in first source	4.28	5	0
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.	3.32	6	0	tripeptide; ureas	antiviral drug; hepatitis C protease inhibitor; peptidomimetic
danoprevir [no description available]	4.29	5	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	3.71	2	0	oligopeptide
simeprevir [no description available]	3	4	0	azamacrocycle; lactam
gs-9451 [no description available]	2.21	1	0
bi 201335 faldaprevir: inhibits hepatitis C virus NS3 protease	4.65	4	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.	4.14	4	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
danoprevir [no description available]	4.08	4	0

Condition	Indicated	Relationship Strength	Studies	Trials
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted [description not available]	0	12.6	21	13
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	14.6	21	13
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.58	2	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Chronic Hepatitis C [description not available]	0	11.62	16	13
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	13.62	16	13
Viremia The presence of viruses in the blood.	0	3.47	1	1
Cirrhosis, Liver [description not available]	0	5.37	2	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	5.37	2	2
Recrudescence [description not available]	0	8.14	5	5
Hepatocellular Carcinoma [description not available]	0	2.06	1	0
Cancer of Liver [description not available]	0	2.06	1	0
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	2.06	1	0
Liver Neoplasms Tumors or cancer of the LIVER.	0	2.06	1	0

mk-7009

Description

Cross-References

Synonyms (32)

Research Excerpts

Toxicity

Bioavailability

Roles (2)

Drug Classes (5)

Protein Targets (31)

Inhibition Measurements

Other Measurements

Biological Processes (129)

Molecular Functions (31)

Ceullar Components (41)

Bioassays (159)

Research

Studies (42)

Market Indicators

Research Demand Index: 16.38

Study Types

mk-7009

Description

Cross-References

Synonyms (32)

Research Excerpts

Toxicity

Bioavailability

Roles (2)

Drug Classes (5)

Protein Targets (31)

Inhibition Measurements

Other Measurements

Biological Processes (129)

Molecular Functions (31)

Ceullar Components (41)

Bioassays (159)

Research

Studies (42)

Market Indicators

Research Demand Index: 16.38

Study Types

Related Drugs (26)

Related Conditions (15)