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Assay Detail

CHEMBL4768523

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

Binding
Inhibition of human recombinant lysosomal GCase using 4-methylumbelliferyl-beta-D-glucopyranoside as substrate preincubated for 45 mins followed by substrate addition and measured after 30 mins by fluorescence spectrophotometric assay
14
Total Activities
14
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

Lysosomal acid glucosylceramidase (CHEMBL2179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of multimeric pyrrolidine iminosugar inhibitors of human β-glucocerebrosidase and α-galactosidase A: First example of a multivalent enzyme activity enhancer for Fabry disease.
Martínez-Bailén M,Carmona AT,Cardona F,Matassini C,Goti A,Kubo M,Kato A,Robina I,Moreno-Vargas AJ
Eur J Med Chem (2020) 192 : 112173 -112173
PubMed 32146376 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.31 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4792854 1 6.60
CHEMBL4783905 1 5.96
CHEMBL4793095 1 5.89
CHEMBL4791125 1 5.54
CHEMBL4779198 1 5.33
CHEMBL4782789 1 5.32
CHEMBL4793871 1 5.16
CHEMBL4218664 1 4.51
CHEMBL4786169 1 4.42
CHEMBL4214414 1 4.41
CHEMBL4795488 1 -
CHEMBL4779093 1 -
CHEMBL4778683 1 -
CHEMBL4794112 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4792854 IC50 = 250.0 nM 6.60
CHEMBL4783905 IC50 = 1100.0 nM 5.96
CHEMBL4793095 IC50 = 1300.0 nM 5.89
CHEMBL4791125 IC50 = 2900.0 nM 5.54
CHEMBL4779198 IC50 = 4700.0 nM 5.33
CHEMBL4782789 IC50 = 4800.0 nM 5.32
CHEMBL4793871 IC50 = 7000.0 nM 5.16
CHEMBL4218664 IC50 = 31000.0 nM 4.51
CHEMBL4786169 IC50 = 38000.0 nM 4.42
CHEMBL4214414 IC50 = 39000.0 nM 4.41
CHEMBL4795488 IC50 = 333000.0 nM -
CHEMBL4779093 IC50 = 168000.0 nM -
CHEMBL4778683 IC50 = 247000.0 nM -
CHEMBL4794112 IC50 = 725000.0 nM -