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Assay Detail

CHEMBL4386780

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of NS5A in HCV genotype 4a ED43 infected in human HuH7 transient chimeric replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 4a
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Nonstructural protein 5A (CHEMBL3307224)
Type SINGLE PROTEIN
Organism Hepatitis C virus

Publication

Discovery of velpatasvir (GS-5816): A potent pan-genotypic HCV NS5A inhibitor in the single-tablet regimens Vosevi<sup>®</sup> and Epclusa<sup>®</sup>.
Link JO, Taylor JG, Trejo-Martin A, Kato D, Katana AA, Krygowski ES, Yang ZY, Zipfel S, Cottell JJ, Bacon EM, Tran CV, Yang CY, Wang Y, Wang KW, Zhao G, Cheng G, Tian Y, Gong R, Lee YJ, Yu M, Gorman E, Mogalian E, Perry JK.
Bioorg Med Chem Lett (2019) 29 : 2415 -2427
PubMed 31230974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 10.68 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4450375 1 10.96
CHEMBL4468617 1 10.96
CHEMBL4574152 1 10.89
CHEMBL4565239 1 10.85
CHEMBL4583723 1 10.82
CHEMBL4457264 1 10.82
CHEMBL4542363 1 10.70
CHEMBL4576714 1 10.66
CHEMBL4436929 1 10.54
CHEMBL4440405 1 10.44
CHEMBL4453135 1 9.89
CHEMBL4536960 1 -
CHEMBL4449384 1 -
CHEMBL4516340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4450375 EC50 = 0.011 nM 10.96
CHEMBL4468617 EC50 = 0.011 nM 10.96
CHEMBL4574152 EC50 = 0.013 nM 10.89
CHEMBL4565239 EC50 = 0.014 nM 10.85
CHEMBL4583723 EC50 = 0.015 nM 10.82
CHEMBL4457264 EC50 = 0.015 nM 10.82
CHEMBL4542363 EC50 = 0.02 nM 10.70
CHEMBL4576714 EC50 = 0.022 nM 10.66
CHEMBL4436929 EC50 = 0.029 nM 10.54
CHEMBL4440405 EC50 = 0.036 nM 10.44
CHEMBL4453135 EC50 = 0.13 nM 9.89
CHEMBL4536960 EC50 = 0.008 nM -
CHEMBL4449384 EC50 = 0.008 nM -
CHEMBL4516340 EC50 = 0.008 nM -