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Assay Detail

CHEMBL2015462

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

Binding
Competitive inhibition of human recombinant beta-glucocerebrosidase assessed as 4-methyumbelliferone formation after 30 mins by Lineweaver-Burk plot analysis at pH 5.2
7
Total Activities
7
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
Ki 7 6.76 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3216319 1 7.58
CHEMBL3216774 1 6.77
CHEMBL408500 1 6.52
CHEMBL2012656 1 6.16
CHEMBL2012659 1 -
CHEMBL2012658 1 -
CHEMBL3216992 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3216319 Ki = 26.0 nM 7.58
CHEMBL3216774 Ki = 170.0 nM 6.77
CHEMBL408500 Ki = 300.0 nM 6.52
CHEMBL2012656 Ki = 700.0 nM 6.16
CHEMBL2012659 Ki - -
CHEMBL2012658 Ki - -
CHEMBL3216992 Ki - -