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Assay Detail

CHEMBL4192278

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

Binding
Inhibition of capsid in HBV infected in human HepAD38 cells assessed as reduction in tetracycline-induced cccDNA formation by measuring reduction in HBe antigen secretion after 14 days by ELISA
14
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis B virus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Core antigen (CHEMBL1075091)
Type SINGLE PROTEIN
Organism Hepatitis B virus

Publication

Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.
Sari O, Boucle S, Cox BD, Ozturk T, Russell OO, Bassit L, Amblard F, Schinazi RF.
Eur J Med Chem (2017) 138 : 407 -421
PubMed 28688280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.59 6.16
EC90 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3742114 2 6.16
CHEMBL4213671 2 6.00
CHEMBL1730444 2 5.89
CHEMBL4204204 2 5.26
CHEMBL4204727 2 5.22
CHEMBL4216398 2 5.01
CHEMBL141 LAMIVUDINE 4.0 1 -
CHEMBL5314362 ENTECAVIR 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3742114 EC50 = 700.0 nM 6.16
CHEMBL4213671 EC50 = 1000.0 nM 6.00
CHEMBL1730444 EC50 = 1300.0 nM 5.89
CHEMBL4204204 EC50 = 5500.0 nM 5.26
CHEMBL4204727 EC50 = 6000.0 nM 5.22
CHEMBL4216398 EC50 = 9700.0 nM 5.01
CHEMBL141 LAMIVUDINE EC50 > 10000.0 nM -
CHEMBL5314362 ENTECAVIR EC50 > 10000.0 nM -
CHEMBL1730444 EC90 = 4.6 uM -
CHEMBL4213671 EC90 = 3.2 uM -
CHEMBL4204204 EC90 > 10.0 uM -
CHEMBL4204727 EC90 > 10.0 uM -
CHEMBL4216398 EC90 > 10.0 uM -
CHEMBL3742114 EC90 = 1.9 uM -