vaniprevir [Ligand Id: 11570] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4525964 (MK-7009, MK7009, Vaniprevir)
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  • chymotrypsin like elastase 1/Elastase 1 in Human [ChEMBL: CHEMBL3000] [GtoPdb: 2338] [UniProtKB: Q9UNI1]
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  • elastase, neutrophil expressed/Leukocyte elastase in Human [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cathepsin F/Cathepsin F in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2517] [GtoPdb: 2347] [UniProtKB: Q9UBX1]
ChEMBL Inhibition of human Cathepsin F B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235]
ChEMBL Inhibition of human Cathepsin K B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
cathepsin V/Cathepsin L2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3272] [GtoPdb: 2352] [UniProtKB: O60911]
ChEMBL Inhibition of human Cathepsin V B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
cathepsin S/Cathepsin S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2954] [GtoPdb: 2353] [UniProtKB: P25774]
ChEMBL Inhibition of human cathepsin S B 4.11 pIC50 78000 nM IC50 Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727]
ChEMBL Inhibition of human Cathepsin S B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
chymase 1/Chymase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4068] [GtoPdb: 2340] [UniProtKB: P23946]
ChEMBL Inhibition of human Chymase B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
chymotrypsin like elastase 1/Elastase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3000] [GtoPdb: 2338] [UniProtKB: Q9UNI1]
ChEMBL Inhibition of human Pancreatic elastase 1 B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
Genome polyprotein in Hepacivirus C (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296298] [UniProtKB: K7XJL6]
ChEMBL Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease A156V mutant expressed in Escherichia coli by time-resolved fluorescence analysis B 7.06 pKi 88 nM Ki ACS Med Chem Lett (2012) 3: 332-336 [PMID:24900473]
ChEMBL Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease D168V mutant expressed in Escherichia coli by time-resolved fluorescence analysis B 7.11 pKi 77 nM Ki ACS Med Chem Lett (2012) 3: 332-336 [PMID:24900473]
ChEMBL Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease A156T mutant expressed in Escherichia coli by time-resolved fluorescence analysis B 7.66 pKi 22 nM Ki ACS Med Chem Lett (2012) 3: 332-336 [PMID:24900473]
Hepatitis C virus serine protease, NS3/NS4A in Hepatitis C virus (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095231] [UniProtKB: A3EZI9D2K2A8]
ChEMBL Inhibition of Hepatitis C virus (isolate BK) genotype 1b NS3/4a protease R155K mutant expressed in Escherichia coli by time-resolved fluorescence analysis B 7.72 pKi 19 nM Ki ACS Med Chem Lett (2012) 3: 332-336 [PMID:24900473]
ChEMBL Inhibition of HCV genotype 1a NS3/4A protease using Ac-DED(Edans)EEAbu-psi[COO]ASK(Dabcyl)-NH2 as substrate by FRET assay B 10.3 pKi 0.05 nM Ki Bioorg Med Chem (2014) 22: 6595-6615 [PMID:25456385]
elastase, neutrophil expressed/Leukocyte elastase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246]
ChEMBL Inhibition of human neutrophil elastase B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727]
ChEMBL Inhibition of human Neutrophil elastase 2 B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Inhibition of human plasmin B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of human thrombin B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727]
serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477]
ChEMBL Inhibition of human Trypsin activity B 5 pIC50 >10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]