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Assay Detail

CHEMBL4841965

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

Functional
Antiviral activity against HBV infected in human HepG2-hNTCP cells assessed as reduction in HBV DNA incubated for day 1 followed by compound washout and fresh compound addition on following day and day 3, 6 and 10 measured on day 14 post infection by qPCR analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Hepatitis B virus
Cell Type HepG2
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Discovery of Modified Amidate (ProTide) Prodrugs of Tenofovir with Enhanced Antiviral Properties.
Kalčic F, Zgarbová M, Hodek J, Chalupský K, Dračínský M, Dvořáková A, Strmeň T, Šebestík J, Baszczyňski O, Weber J, Mertlíková-Kaiserová H, Janeba Z.
J Med Chem (2021) 64 : 16425 -16449
PubMed 34713696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.69 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875146 1 9.70
CHEMBL4859319 1 9.57
CHEMBL4878556 1 9.22
CHEMBL4869422 1 9.15
CHEMBL4854971 1 8.92
CHEMBL4865455 1 8.89
CHEMBL4868959 1 8.85
CHEMBL4855770 1 8.85
CHEMBL4863664 1 8.80
CHEMBL4877554 1 8.55
CHEMBL4877971 1 8.49
CHEMBL4849286 1 8.47
CHEMBL4864042 1 8.44
CHEMBL4849197 1 8.40
CHEMBL4859604 1 8.38
CHEMBL4873511 1 8.36
CHEMBL2364637 TENOFOVIR ALAFENAMIDE FUMARATE 4.0 1 8.28
CHEMBL4855762 1 8.14
CHEMBL4877392 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875146 EC50 = 0.2 nM 9.70
CHEMBL4859319 EC50 = 0.27 nM 9.57
CHEMBL4878556 EC50 = 0.6 nM 9.22
CHEMBL4869422 EC50 = 0.7 nM 9.15
CHEMBL4854971 EC50 = 1.2 nM 8.92
CHEMBL4865455 EC50 = 1.3 nM 8.89
CHEMBL4868959 EC50 = 1.4 nM 8.85
CHEMBL4855770 EC50 = 1.4 nM 8.85
CHEMBL4863664 EC50 = 1.6 nM 8.80
CHEMBL4877554 EC50 = 2.8 nM 8.55
CHEMBL4877971 EC50 = 3.2 nM 8.49
CHEMBL4849286 EC50 = 3.4 nM 8.47
CHEMBL4864042 EC50 = 3.6 nM 8.44
CHEMBL4849197 EC50 = 4.0 nM 8.40
CHEMBL4859604 EC50 = 4.2 nM 8.38
CHEMBL4873511 EC50 = 4.4 nM 8.36
CHEMBL2364637 TENOFOVIR ALAFENAMIDE FUMARATE EC50 = 5.3 nM 8.28
CHEMBL4855762 EC50 = 7.2 nM 8.14
CHEMBL4877392 EC50 = 19.0 nM 7.72