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Assay Detail

CHEMBL4394392

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

Binding
Inhibition of HCV NS5B RNA-dependent RNA polymerase activity assessed as reduction in radiolabeled-UTP incorporation into RNA using cIRES template measured after 2 hrs by microscintillation counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and Anti-HCV Activities of 4'-Fluoro-2'-Substituted Uridine Triphosphates and Nucleotide Prodrugs: Discovery of 4'-Fluoro-2'- C-methyluridine 5'-Phosphoramidate Prodrug (AL-335) for the Treatment of Hepatitis C Infection.
Wang G, Dyatkina N, Prhavc M, Williams C, Serebryany V, Hu Y, Huang Y, Wan J, Wu X, Deval J, Fung A, Jin Z, Tan H, Shaw K, Kang H, Zhang Q, Tam Y, Stoycheva A, Jekle A, Smith DB, Beigelman L.
J Med Chem (2019) 62 : 4555 -4570
PubMed 30951311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.44 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127092 1 7.57
CHEMBL4125966 1 7.41
CHEMBL4555315 1 6.96
CHEMBL4127030 ADAFOSBUVIR 5'-TRIPHOSPHATE -1.0 1 6.85
CHEMBL4543543 1 6.82
CHEMBL4592496 1 6.72
CHEMBL4592592 1 6.55
CHEMBL4088430 1 6.52
CHEMBL4127921 1 6.48
CHEMBL4454742 1 6.47
CHEMBL4440367 1 6.07
CHEMBL4522072 1 5.19
CHEMBL4546003 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127092 IC50 = 27.0 nM 7.57
CHEMBL4125966 IC50 = 39.0 nM 7.41
CHEMBL4555315 IC50 = 110.0 nM 6.96
CHEMBL4127030 ADAFOSBUVIR 5'-TRIPHOSPHATE IC50 = 140.0 nM 6.85
CHEMBL4543543 IC50 = 150.0 nM 6.82
CHEMBL4592496 IC50 = 190.0 nM 6.72
CHEMBL4592592 IC50 = 280.0 nM 6.55
CHEMBL4088430 IC50 = 300.0 nM 6.52
CHEMBL4127921 IC50 = 330.0 nM 6.48
CHEMBL4454742 IC50 = 340.0 nM 6.47
CHEMBL4440367 IC50 = 860.0 nM 6.07
CHEMBL4522072 IC50 = 6400.0 nM 5.19
CHEMBL4546003 IC50 = 84000.0 nM 4.08