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Assay Detail

CHEMBL1768947

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

Binding
Inhibition of recombinant glucocerebrosidase in McIlvaine buffer at pH 7.4 after 10 mins by fluorometric analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

New glucocerebrosidase inhibitors by exploration of chemical diversity of N-substituted aminocyclitols using click chemistry and in situ screening.
Díaz L, Casas J, Bujons J, Llebaria A, Delgado A.
J Med Chem (2011) 54 : 2069 -2079
PubMed 21370884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.37 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766350 1 7.22
CHEMBL1766482 1 7.00
CHEMBL1766474 1 6.52
CHEMBL408500 1 6.52
CHEMBL1766489 1 5.89
CHEMBL1766470 1 5.75
CHEMBL1766473 1 5.72
CHEMBL1083795 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766350 IC50 = 60.0 nM 7.22
CHEMBL1766482 IC50 = 100.0 nM 7.00
CHEMBL1766474 IC50 = 300.0 nM 6.52
CHEMBL408500 IC50 = 300.0 nM 6.52
CHEMBL1766489 IC50 = 1300.0 nM 5.89
CHEMBL1766470 IC50 = 1800.0 nM 5.75
CHEMBL1766473 IC50 = 1900.0 nM 5.72
CHEMBL1083795 IC50 - -