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Assay Detail

CHEMBL854142

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

Binding
Inhibitory activity against HCV 1b BK NS5B deltaC55 RNA polymerase involving magnesium chelation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1b
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis.
Koch U, Attenni B, Malancona S, Colarusso S, Conte I, Di Filippo M, Harper S, Pacini B, Giomini C, Thomas S, Incitti I, Tomei L, De Francesco R, Altamura S, Matassa VG, Narjes F.
J Med Chem (2006) 49 : 1693 -1705
PubMed 16509585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.76 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175882 1 6.82
CHEMBL382170 1 6.17
CHEMBL382383 1 6.12
CHEMBL203575 1 5.92
CHEMBL181653 1 5.58
CHEMBL205026 1 5.54
CHEMBL366051 1 5.38
CHEMBL440562 1 4.52
CHEMBL203976 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175882 IC50 = 150.0 nM 6.82
CHEMBL382170 IC50 = 680.0 nM 6.17
CHEMBL382383 IC50 = 760.0 nM 6.12
CHEMBL203575 IC50 = 1200.0 nM 5.92
CHEMBL181653 IC50 = 2600.0 nM 5.58
CHEMBL205026 IC50 = 2900.0 nM 5.54
CHEMBL366051 IC50 = 4200.0 nM 5.38
CHEMBL440562 IC50 = 30000.0 nM 4.52
CHEMBL203976 IC50 > 50000.0 nM -