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Assay Detail

CHEMBL4059401

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

Binding
Inhibition of human CathA-IRES-6His-tagged NEU1 expressed in HEK293T cells using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by fluorescence based assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sialidase-1 (CHEMBL2726)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Inhibitors of Human Neuraminidase 3.
Guo T, Dätwyler P, Demina E, Richards MR, Ge P, Zou C, Zheng R, Fougerat A, Pshezhetsky AV, Ernst B, Cairo CW.
J Med Chem (2018) 61 : 1990 -2008
PubMed 29425031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 4.21 4.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060974 1 4.33
CHEMBL96712 NEU5AC2EN 1 4.31
CHEMBL4089157 1 4.29
CHEMBL4076383 1 4.23
CHEMBL4084911 1 4.12
CHEMBL4096864 1 4.00
CHEMBL4093209 1 -
CHEMBL4075574 1 -
CHEMBL4084317 1 -
CHEMBL4100761 1 -
CHEMBL4073992 1 -
CHEMBL4081811 1 -
CHEMBL4099818 1 -
CHEMBL4064112 1 -
CHEMBL4062382 1 -
CHEMBL4063782 1 -
CHEMBL4071732 1 -
CHEMBL4069646 1 -
CHEMBL4080360 1 -
CHEMBL222813 ZANAMIVIR 4.0 1 -
CHEMBL4076203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060974 IC50 = 47000.0 nM 4.33
CHEMBL96712 NEU5AC2EN IC50 = 49000.0 nM 4.31
CHEMBL4089157 IC50 = 51000.0 nM 4.29
CHEMBL4076383 IC50 = 59000.0 nM 4.23
CHEMBL4084911 IC50 = 76000.0 nM 4.12
CHEMBL4096864 IC50 = 100000.0 nM 4.00
CHEMBL4093209 IC50 > 500000.0 nM -
CHEMBL4075574 IC50 > 500000.0 nM -
CHEMBL4084317 IC50 > 500000.0 nM -
CHEMBL4100761 IC50 > 500000.0 nM -
CHEMBL4073992 IC50 > 500000.0 nM -
CHEMBL4081811 IC50 > 500000.0 nM -
CHEMBL4099818 IC50 > 500000.0 nM -
CHEMBL4064112 IC50 > 500000.0 nM -
CHEMBL4062382 IC50 > 500000.0 nM -
CHEMBL4063782 IC50 > 500000.0 nM -
CHEMBL4071732 IC50 = 240000.0 nM -
CHEMBL4069646 IC50 = 140000.0 nM -
CHEMBL4080360 IC50 = 190000.0 nM -
CHEMBL222813 ZANAMIVIR IC50 > 500000.0 nM -
CHEMBL4076203 IC50 > 500000.0 nM -