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Assay Detail

CHEMBL4432409

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

Binding
Inhibition of HCV genotype 1b Con1 NS5B RNA dependent RNA polymerase
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus (isolate Con1)
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Genome polyprotein (CHEMBL5536)
Type SINGLE PROTEIN
Organism Hepatitis C virus genotype 1b (isolate Con1) (HCV)

Publication

Synthesis of potent and broad genotypically active NS5B HCV non-nucleoside inhibitors binding to the thumb domain allosteric site 2 of the viral polymerase.
Pierra Rouvière C, Amador A, Badaroux E, Convard T, Da Costa D, Dukhan D, Griffe L, Griffon JF, LaColla M, Leroy F, Liuzzi M, Loi AG, McCarville J, Mascia V, Milhau J, Onidi L, Paparin JL, Rahali R, Sais E, Seifer M, Surleraux D, Standring D, Dousson C.
Bioorg Med Chem Lett (2016) 26 : 4536 -4541
PubMed 27520942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.79 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527971 1 8.05
CHEMBL4441238 3 8.00
CHEMBL4444480 1 7.84
CHEMBL4545438 1 7.79
CHEMBL4593826 1 7.75
CHEMBL4471005 1 7.60
CHEMBL4548240 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527971 IC50 = 9.0 nM 8.05
CHEMBL4441238 IC50 = 9.9 nM 8.00
CHEMBL4441238 IC50 = 12.7 nM 7.90
CHEMBL4444480 IC50 = 14.3 nM 7.84
CHEMBL4545438 IC50 = 16.3 nM 7.79
CHEMBL4593826 IC50 = 18.0 nM 7.75
CHEMBL4441238 IC50 = 18.5 nM 7.73
CHEMBL4471005 IC50 = 25.3 nM 7.60
CHEMBL4548240 IC50 = 33.5 nM 7.47