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Assay Detail

CHEMBL1786572

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

Binding
Inhibition of Hepatitis C virus subtype 1b NS5B activity assessed as inhibition of poly(A)n.oligo(dT)12-18-directed incorporation of [3H]-UTP into DNA after 45 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 1b
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

The synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid hepatitis C virus polymerase NS5B inhibitors.
Martin SW, Glunz P, Beno BR, Bergstrom C, Romine JL, Priestley ES, Newman M, Gao M, Roberts S, Rigat K, Fridell R, Qiu D, Knobloh G, Wang YK.
Bioorg Med Chem Lett (2011) 21 : 2869 -2872
PubMed 21507645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.99 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1784254 1 6.47
CHEMBL1784248 1 6.42
CHEMBL1784250 1 6.36
CHEMBL1784249 1 6.34
CHEMBL211639 1 6.19
CHEMBL1784251 1 6.19
CHEMBL1784239 1 6.10
CHEMBL1784253 1 6.09
CHEMBL1784252 1 5.99
CHEMBL1784246 1 5.79
CHEMBL1784255 1 5.64
CHEMBL1784256 1 5.57
CHEMBL1784247 1 5.39
CHEMBL1784257 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1784254 IC50 = 340.0 nM 6.47
CHEMBL1784248 IC50 = 380.0 nM 6.42
CHEMBL1784250 IC50 = 440.0 nM 6.36
CHEMBL1784249 IC50 = 460.0 nM 6.34
CHEMBL211639 IC50 = 640.0 nM 6.19
CHEMBL1784251 IC50 = 650.0 nM 6.19
CHEMBL1784239 IC50 = 790.0 nM 6.10
CHEMBL1784253 IC50 = 820.0 nM 6.09
CHEMBL1784252 IC50 = 1030.0 nM 5.99
CHEMBL1784246 IC50 = 1620.0 nM 5.79
CHEMBL1784255 IC50 = 2290.0 nM 5.64
CHEMBL1784256 IC50 = 2700.0 nM 5.57
CHEMBL1784247 IC50 = 4030.0 nM 5.39
CHEMBL1784257 IC50 = 5200.0 nM 5.28