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Assay Detail

CHEMBL4730979

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

Functional
Antiviral activity against Hepatitis B virus infected in human HepaRG cells assessed as inhibition of HBV DNA replication under CYP450 restriction pre-treated for 1 hr with CYP450 inhibitors ABT and SKF-525A on day 5 post-infection followed by removal of media and supplemented with fresh media containing diluted compound and further incubated for 3 days then followed by treatment for 1 hr with CYP450 inhibitors ABT and SKF-525A on day 8 post-infection followed by removal of media and supplemented with fresh media containing diluted compound and further incubated for 3 days in presence of 25 uM SKF-525A and measured on day 11 post-infection by chemiluminescence immunostaining assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepatitis B virus
Cell Type HepaRG
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatitis B virus (CHEMBL613497)
Type ORGANISM
Organism Hepatitis B virus

Publication

P450s under Restriction (PURE) Screen Using HepaRG and Primary Human Hepatocytes for Discovery of Novel HBV Antivirals.
Hartman GD,Kuduk SD,Espiritu C,Lam AM
ACS Med Chem Lett (2020) 11 : 1919 -1927
PubMed 33062174 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.84 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3742114 1 7.96
CHEMBL4796398 1 6.70
CHEMBL605300 1 6.58
CHEMBL316306 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3742114 EC50 = 11.0 nM 7.96
CHEMBL4796398 EC50 = 200.0 nM 6.70
CHEMBL605300 EC50 = 260.0 nM 6.58
CHEMBL316306 EC50 = 780.0 nM 6.11