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Assay Detail

CHEMBL3363103

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

Functional
Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as inhibition of NS4A expression by ELISA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepacivirus hominis
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis C virus (CHEMBL379)
Type ORGANISM
Organism Hepacivirus hominis

Publication

Structure-based design of a novel series of azetidine inhibitors of the hepatitis C virus NS3/4A serine protease.
Parsy C, Alexandre FR, Brandt G, Caillet C, Cappelle S, Chaves D, Convard T, Derock M, Gloux D, Griffon Y, Lallos L, Leroy F, Liuzzi M, Loi AG, Moulat L, Musiu C, Rahali H, Roques V, Seifer M, Standring D, Surleraux D.
Bioorg Med Chem Lett (2014) 24 : 4444 -4449
PubMed 25155387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.84 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297884 CILUPREVIR 2.0 1 8.55
CHEMBL3326829 1 7.35
CHEMBL3326830 1 7.22
CHEMBL3326539 1 6.62
CHEMBL3326826 1 6.38
CHEMBL3326540 1 6.06
CHEMBL3326538 1 5.73
CHEMBL3326536 1 -
CHEMBL3326537 1 -
CHEMBL3326827 1 -
CHEMBL3326828 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297884 CILUPREVIR EC50 = 2.8 nM 8.55
CHEMBL3326829 EC50 = 45.0 nM 7.35
CHEMBL3326830 EC50 = 60.0 nM 7.22
CHEMBL3326539 EC50 = 242.0 nM 6.62
CHEMBL3326826 EC50 = 412.5 nM 6.38
CHEMBL3326540 EC50 = 871.7 nM 6.06
CHEMBL3326538 EC50 = 1860.0 nM 5.73
CHEMBL3326536 EC50 - -
CHEMBL3326537 EC50 - -
CHEMBL3326827 EC50 < 750.0 nM -
CHEMBL3326828 EC50 < 750.0 nM -