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Assay Detail

CHEMBL4276022

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

Binding
Inhibition of beta-glucosidase derived from human peripheral blood mononuclear cell lysate using 4-methylumbelliferyl beta-D-glucopyranoside as substrate after 2 hrs by fluorescence analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-glucosidase (CHEMBL3761)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-epi-Isofagomine derivatives as pharmacological chaperones for the treatment of lysosomal diseases linked to β-galactosidase mutations: Improved synthesis and biological investigations.
Front S, Almeida S, Zoete V, Charollais-Thoenig J, Gallienne E, Marmy C, Pilloud V, Marti R, Wood T, Martin OR, Demotz S.
Bioorg Med Chem (2018) 26 : 5462 -5469
PubMed 30270003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.28 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206468 AFEGOSTAT 2.0 1 7.70
CHEMBL4288931 1 7.40
CHEMBL4085739 1 5.00
CHEMBL4284436 1 5.00
CHEMBL4281031 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL206468 AFEGOSTAT IC50 = 20.0 nM 7.70
CHEMBL4288931 IC50 = 40.0 nM 7.40
CHEMBL4085739 IC50 = 10000.0 nM 5.00
CHEMBL4284436 IC50 = 10000.0 nM 5.00
CHEMBL4281031 IC50 > 10000.0 nM -