velpatasvir [Ligand Id: 11269] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3545062 (GS-5816, Velpatasvir)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Nonstructural protein 5A in Hepatitis C virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3307224] [UniProtKB: Q5L478]
ChEMBL Inhibition of NS5A Y93H mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 8.07 pEC50 8.5 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93H mutant in HCV genotype 3a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 8.49 pEC50 3.2 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Q30E mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.6 pEC50 0.25 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A L31M mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.66 pEC50 0.22 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A A30K mutant in HCV genotype 3a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.68 pEC50 0.21 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 6e D88 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.89 pEC50 0.13 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A M28T mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 9.98 pEC50 0.1 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 5a SA13 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.27 pEC50 0.05 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93C mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.28 pEC50 0.05 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Q30H mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.49 pEC50 0.03 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Q30R mutant in HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.51 pEC50 0.03 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 1b Con1 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.8 pEC50 0.02 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A L31M mutant in HCV genotype 2a J6 (M31) infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.8 pEC50 0.02 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 1b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.8 pEC50 0.02 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 2a J6 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.8 pEC50 0.02 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.85 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 1a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.85 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A in wild type HCV genotype 3a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.89 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A R44K mutant in HCV genotype 2b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.96 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A Y93H mutant in HCV genotype 1b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 10.96 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A P58S mutant in HCV genotype 2b infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 11 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]
ChEMBL Inhibition of NS5A N62V mutant in HCV genotype 2a infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay B 11 pEC50 0.01 nM EC50 Bioorg Med Chem Lett (2019) 29: 2415-2427 [PMID:31230974]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]