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Assay Detail

CHEMBL4627976

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

Binding
Inhibition of NS5B polymerase in HCV genotype 1a H77 infected in human HuH7 replicon cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1a
Cell Type Huh-7
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of 2-aminoisobutyric acid ethyl ester (AIBEE) phosphoramidate prodrugs for delivering nucleoside HCV NS5B polymerase inhibitors.
Randolph JT, Li T, Chris Krueger A, Heyman HR, Chen HJ, Bow DAJ, Van Handel C, Peterkin V, Carr RA, Stolarik D, Dekhtyar T, Irvin M, Krishnan P, Wagner R, DeGoey DA.
Bioorg Med Chem Lett (2020) 30 : 126986 -126986
PubMed 32046903 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.47 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635092 1 7.03
CHEMBL4647104 1 7.01
CHEMBL4641335 1 6.97
CHEMBL4636436 1 6.94
CHEMBL1259059 SOFOSBUVIR 4.0 1 6.81
CHEMBL4639827 1 6.81
CHEMBL4644488 1 6.53
CHEMBL4633686 1 6.50
CHEMBL4639671 1 6.38
CHEMBL4642954 1 6.38
CHEMBL4644867 1 6.23
CHEMBL4635910 1 6.02
CHEMBL4634173 1 5.96
CHEMBL4637964 1 5.92
CHEMBL4640222 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635092 EC50 = 94.0 nM 7.03
CHEMBL4647104 EC50 = 98.0 nM 7.01
CHEMBL4641335 EC50 = 106.0 nM 6.97
CHEMBL4636436 EC50 = 114.0 nM 6.94
CHEMBL1259059 SOFOSBUVIR EC50 = 155.0 nM 6.81
CHEMBL4639827 EC50 = 156.0 nM 6.81
CHEMBL4644488 EC50 = 298.0 nM 6.53
CHEMBL4633686 EC50 = 317.0 nM 6.50
CHEMBL4639671 EC50 = 415.0 nM 6.38
CHEMBL4642954 EC50 = 414.0 nM 6.38
CHEMBL4644867 EC50 = 592.0 nM 6.23
CHEMBL4635910 EC50 = 960.0 nM 6.02
CHEMBL4634173 EC50 = 1090.0 nM 5.96
CHEMBL4637964 EC50 = 1210.0 nM 5.92
CHEMBL4640222 EC50 = 2500.0 nM 5.60