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Assay Detail

CHEMBL2015461

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

Binding
Inhibition of human recombinant beta-glucocerebrosidase assessed as 4-methyumbelliferone formation after 30 mins by spectrophotometric analysis at pH 5.2
6
Total Activities
6
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

The myo-1,2-Diaminocyclitol Scaffold Defines Potent Glucocerebrosidase Activators and Promising Pharmacological Chaperones for Gaucher Disease.
Trapero A, Llebaria A.
ACS Med Chem Lett (2011) 2 : 614 -619
PubMed 24900357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.90 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3216319 1 7.05
CHEMBL3216774 1 6.19
CHEMBL408500 1 6.18
CHEMBL2012656 1 5.79
CHEMBL3216992 1 4.27
CHEMBL2012659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3216319 IC50 = 90.0 nM 7.05
CHEMBL3216774 IC50 = 640.0 nM 6.19
CHEMBL408500 IC50 = 660.0 nM 6.18
CHEMBL2012656 IC50 = 1610.0 nM 5.79
CHEMBL3216992 IC50 = 53400.0 nM 4.27
CHEMBL2012659 IC50 = 144000.0 nM -