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Assay Detail

CHEMBL4386718

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

Binding
Inhibition of NS5A in HCV genotype 2a JFH1 (L31) infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 2a
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 21 10.42 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4575259 1 11.00
CHEMBL4580476 1 10.85
CHEMBL4579101 1 10.85
CHEMBL4453135 1 10.80
CHEMBL4466791 1 10.80
CHEMBL4533239 1 10.72
CHEMBL4550389 1 10.70
CHEMBL4458486 1 10.70
CHEMBL4437973 1 10.66
CHEMBL4588951 1 10.66
CHEMBL4442040 1 10.42
CHEMBL4466693 1 10.14
CHEMBL4542747 1 10.13
CHEMBL3914296 1 9.88
CHEMBL4469219 1 9.65
CHEMBL4588138 1 8.83
CHEMBL4466184 1 -
CHEMBL4543321 1 -
CHEMBL4562949 1 -
CHEMBL4436929 1 -
CHEMBL4536960 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4575259 EC50 = 0.01 nM 11.00
CHEMBL4580476 EC50 = 0.014 nM 10.85
CHEMBL4579101 EC50 = 0.014 nM 10.85
CHEMBL4453135 EC50 = 0.016 nM 10.80
CHEMBL4466791 EC50 = 0.016 nM 10.80
CHEMBL4533239 EC50 = 0.019 nM 10.72
CHEMBL4550389 EC50 = 0.02 nM 10.70
CHEMBL4458486 EC50 = 0.02 nM 10.70
CHEMBL4437973 EC50 = 0.022 nM 10.66
CHEMBL4588951 EC50 = 0.022 nM 10.66
CHEMBL4442040 EC50 = 0.038 nM 10.42
CHEMBL4466693 EC50 = 0.073 nM 10.14
CHEMBL4542747 EC50 = 0.074 nM 10.13
CHEMBL3914296 EC50 = 0.131 nM 9.88
CHEMBL4469219 EC50 = 0.223 nM 9.65
CHEMBL4588138 EC50 = 1.47 nM 8.83
CHEMBL4466184 EC50 = 0.007 nM -
CHEMBL4543321 EC50 = 0.004 nM -
CHEMBL4562949 EC50 = 0.009 nM -
CHEMBL4436929 EC50 = 0.007 nM -
CHEMBL4536960 EC50 = 0.004 nM -