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Assay Detail

CHEMBL2172827

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

Binding
Inhibition of wild type glucocerebrosidase in human spleen homogenate using 4-methylumbellifereno-Glc as substrate incubated for 5 mins prior to substrate addition measured after 20 mins by fluorimetric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Spleen
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery, structure-activity relationship, and biological evaluation of noninhibitory small molecule chaperones of glucocerebrosidase.
Patnaik S, Zheng W, Choi JH, Motabar O, Southall N, Westbroek W, Lea WA, Velayati A, Goldin E, Sidransky E, Leister W, Marugan JJ.
J Med Chem (2012) 55 : 5734 -5748
PubMed 22646221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.85 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1361379 1 6.55
CHEMBL103769 1 6.44
CHEMBL403714 1 5.66
CHEMBL406121 1 5.50
CHEMBL429079 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1361379 IC50 = 280.0 nM 6.55
CHEMBL103769 IC50 = 360.0 nM 6.44
CHEMBL403714 IC50 = 2200.0 nM 5.66
CHEMBL406121 IC50 = 3200.0 nM 5.50
CHEMBL429079 IC50 = 7900.0 nM 5.10