Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4768524

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

Binding
Competitive 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 spectrophotometry based Lineweaver-Burk plot analysis
10
Total Activities
10
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
Ki 10 5.35 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4792854 1 6.11
CHEMBL4783905 1 5.96
CHEMBL4793095 1 5.92
CHEMBL4791125 1 5.80
CHEMBL4782789 1 5.58
CHEMBL4779198 1 5.57
CHEMBL4793871 1 5.27
CHEMBL4218664 1 4.72
CHEMBL4214414 1 4.26
CHEMBL4786169 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4792854 Ki = 770.0 nM 6.11
CHEMBL4783905 Ki = 1100.0 nM 5.96
CHEMBL4793095 Ki = 1200.0 nM 5.92
CHEMBL4791125 Ki = 1600.0 nM 5.80
CHEMBL4782789 Ki = 2600.0 nM 5.58
CHEMBL4779198 Ki = 2700.0 nM 5.57
CHEMBL4793871 Ki = 5400.0 nM 5.27
CHEMBL4218664 Ki = 19000.0 nM 4.72
CHEMBL4214414 Ki = 55000.0 nM 4.26
CHEMBL4786169 Ki = 55000.0 nM 4.26