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Assay Detail

CHEMBL4386717

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

Binding
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
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 6e
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 4 8.84 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4588741 1 9.96
CHEMBL3545062 VELPATASVIR 4.0 1 9.89
CHEMBL4436929 1 8.94
CHEMBL2374220 LEDIPASVIR 4.0 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4588741 EC50 = 0.11 nM 9.96
CHEMBL3545062 VELPATASVIR EC50 = 0.13 nM 9.89
CHEMBL4436929 EC50 = 1.16 nM 8.94
CHEMBL2374220 LEDIPASVIR EC50 = 264.0 nM 6.58