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Assay Detail

CHEMBL5152176

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

Binding
Inhibition of Influenza A virus A/Anhui/1/2005 (H5N1) Neuraminidase H274Y mutant using 2(4-methylurnbellifery1)-a-u-acetyl neuraminic acid sodium salt hydrate (4-MUNANA) as substrate preincubated for 10 mins followed by substrate addition and measured after 40 mins by fluorescence based microplate reader method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Influenza A virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuraminidase (CHEMBL1667685)
Type SINGLE PROTEIN
Organism Influenza A virus

Publication

Identification of C5-NH<sub>2</sub> Modified Oseltamivir Derivatives as Novel Influenza Neuraminidase Inhibitors with Highly Improved Antiviral Activities and Favorable Druggability.
Ju H, Murugan NA, Hou L, Li P, Guizzo L, Zhang Y, Bertagnin C, Kong X, Kang D, Jia R, Ma X, Du R, Poongavanam V, Loregian A, Huang B, Liu X, Zhan P.
J Med Chem (2021) 64 : 17992 -18009
PubMed 34735766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.31 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222813 ZANAMIVIR 4.0 1 8.02
CHEMBL5207634 1 5.36
CHEMBL5181864 1 5.19
CHEMBL674 OSELTAMIVIR CARBOXYLATE -1.0 1 5.08
CHEMBL5193354 1 4.67
CHEMBL5172128 1 4.58
CHEMBL5181442 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222813 ZANAMIVIR IC50 = 9.6 nM 8.02
CHEMBL5207634 IC50 = 4370.0 nM 5.36
CHEMBL5181864 IC50 = 6500.0 nM 5.19
CHEMBL674 OSELTAMIVIR CARBOXYLATE IC50 = 8260.0 nM 5.08
CHEMBL5193354 IC50 = 21300.0 nM 4.67
CHEMBL5172128 IC50 = 26500.0 nM 4.58
CHEMBL5181442 IC50 = 51300.0 nM 4.29