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Assay Detail

CHEMBL4261237

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

Binding
Inhibition of MBP-fused human NEU4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sialidase-4 (CHEMBL4174)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Inhibitors of Human Neuraminidase 1 (NEU1).
Guo T, Héon-Roberts R, Zou C, Zheng R, Pshezhetsky AV, Cairo CW.
J Med Chem (2018) 61 : 11261 -11279
PubMed 30457869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 4.50 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285561 1 5.58
CHEMBL1289862 1 5.25
CHEMBL4288490 1 5.08
CHEMBL96712 NEU5AC2EN 1 5.08
CHEMBL4279510 1 4.62
CHEMBL4292800 1 4.44
CHEMBL4277615 1 4.34
CHEMBL4277689 1 4.33
CHEMBL4277321 1 4.28
CHEMBL3558288 1 4.15
CHEMBL4289116 1 4.13
CHEMBL4281100 1 4.09
CHEMBL4277834 1 4.06
CHEMBL4291435 1 4.06
CHEMBL4277391 1 4.00
CHEMBL4293651 1 -
CHEMBL4283057 1 -
CHEMBL4290253 1 -
CHEMBL4279593 1 -
CHEMBL4286830 1 -
CHEMBL4294730 1 -
CHEMBL4283482 1 -
CHEMBL4291325 1 -
CHEMBL4281290 1 -
CHEMBL4291908 1 -
CHEMBL4290845 1 -
CHEMBL4289583 1 -
CHEMBL4287431 1 -
CHEMBL4280607 1 -
CHEMBL4295174 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285561 IC50 = 2600.0 nM 5.58
CHEMBL1289862 IC50 = 5600.0 nM 5.25
CHEMBL96712 NEU5AC2EN IC50 = 8300.0 nM 5.08
CHEMBL4288490 IC50 = 8400.0 nM 5.08
CHEMBL4279510 IC50 = 24000.0 nM 4.62
CHEMBL4292800 IC50 = 36000.0 nM 4.44
CHEMBL4277615 IC50 = 46000.0 nM 4.34
CHEMBL4277689 IC50 = 47000.0 nM 4.33
CHEMBL4277321 IC50 = 52000.0 nM 4.28
CHEMBL3558288 IC50 = 71000.0 nM 4.15
CHEMBL4289116 IC50 = 74000.0 nM 4.13
CHEMBL4281100 IC50 = 81000.0 nM 4.09
CHEMBL4277834 IC50 = 87000.0 nM 4.06
CHEMBL4291435 IC50 = 87000.0 nM 4.06
CHEMBL4277391 IC50 = 100000.0 nM 4.00
CHEMBL4294661 IC50 = 150000.0 nM -
CHEMBL4290966 IC50 > 500000.0 nM -
CHEMBL4291251 IC50 = 230000.0 nM -
CHEMBL4286541 IC50 = 310000.0 nM -
CHEMBL4294428 IC50 = 290000.0 nM -
CHEMBL4076483 IC50 = 220000.0 nM -
CHEMBL4284515 IC50 = 370000.0 nM -
CHEMBL4284646 IC50 > 500000.0 nM -
CHEMBL4292528 IC50 = 400000.0 nM -
CHEMBL4288030 IC50 = 300000.0 nM -
CHEMBL4280792 IC50 = 110000.0 nM -
CHEMBL4278858 IC50 = 130000.0 nM -
CHEMBL4291991 IC50 > 500000.0 nM -
CHEMBL4291733 IC50 = 150000.0 nM -
CHEMBL4277681 IC50 > 500000.0 nM -
CHEMBL1289198 IC50 = 150000.0 nM -
CHEMBL4293651 IC50 > 500000.0 nM -
CHEMBL4283057 IC50 = 270000.0 nM -
CHEMBL4290253 IC50 = 170000.0 nM -
CHEMBL4279593 IC50 > 500000.0 nM -
CHEMBL4286830 IC50 = 210000.0 nM -
CHEMBL4294730 IC50 = 190000.0 nM -
CHEMBL4283482 IC50 > 500000.0 nM -
CHEMBL4291325 IC50 > 500000.0 nM -
CHEMBL4281290 IC50 = 110000.0 nM -
CHEMBL4291908 IC50 = 440000.0 nM -
CHEMBL4290845 IC50 = 150000.0 nM -
CHEMBL4289583 IC50 = 470000.0 nM -
CHEMBL4287431 IC50 = 210000.0 nM -
CHEMBL4280607 IC50 = 130000.0 nM -
CHEMBL4295174 IC50 > 500000.0 nM -