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Assay Detail

CHEMBL4413706

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

Binding
Inhibition of NS5B polymerase in HCV genotype 2a infected in human HuH7 replicon cells after 5 days by RT-PCR analysis
6
Total Activities
3
Compounds Tested
2
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

RNA-directed RNA polymerase (CHEMBL4296320)
Type SINGLE PROTEIN
Organism Hepacivirus hominis

Publication

Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
Mengshetti S, Zhou L, Sari O, De Schutter C, Zhang H, Cho JH, Tao S, Bassit LC, Verma K, Domaoal RA, Ehteshami M, Jiang Y, Ovadia R, Kasthuri M, Ollinger Russell O, McBrayer T, Whitaker T, Pattassery J, Pascual ML, Uher L, Lin BY, Lee S, Amblard F, Coats SJ, Schinazi RF.
J Med Chem (2019) 62 : 1859 -1874
PubMed 30653317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.17 7.37
EC90 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1259059 SOFOSBUVIR 4.0 2 7.37
CHEMBL4455349 2 7.34
CHEMBL4469773 2 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1259059 SOFOSBUVIR EC50 = 43.0 nM 7.37
CHEMBL4455349 EC50 = 46.0 nM 7.34
CHEMBL4469773 EC50 = 160.0 nM 6.80
CHEMBL4469773 EC90 = 0.83 uM -
CHEMBL4455349 EC90 = 0.077 uM -
CHEMBL1259059 SOFOSBUVIR EC90 = 0.13 uM -