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Assay Detail

CHEMBL2168214

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

Binding
Competitive inhibition of recombinant Imiglucerase using 4-methylumbelliferyl-beta-D-glucopyranoside as substrate preincubated for 30 mins before substrate addition at pH 7.0 by Dixon plot assay
10
Total Activities
10
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

Potent aminocyclitol glucocerebrosidase inhibitors are subnanomolar pharmacological chaperones for treating gaucher disease.
Trapero A, González-Bulnes P, Butters TD, Llebaria A.
J Med Chem (2012) 55 : 4479 -4488
PubMed 22512696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.70 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164231 1 8.30
CHEMBL2164230 1 7.72
CHEMBL2164227 1 7.60
CHEMBL2164232 1 6.92
CHEMBL2164229 1 6.77
CHEMBL408500 1 6.52
CHEMBL2164233 1 6.28
CHEMBL2164228 1 6.17
CHEMBL2163840 1 6.11
CHEMBL2163841 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164231 IC50 = 5.0 nM 8.30
CHEMBL2164230 IC50 = 19.0 nM 7.72
CHEMBL2164227 IC50 = 25.0 nM 7.60
CHEMBL2164232 IC50 = 120.0 nM 6.92
CHEMBL2164229 IC50 = 170.0 nM 6.77
CHEMBL408500 IC50 = 300.0 nM 6.52
CHEMBL2164233 IC50 = 530.0 nM 6.28
CHEMBL2164228 IC50 = 670.0 nM 6.17
CHEMBL2163840 IC50 = 780.0 nM 6.11
CHEMBL2163841 IC50 = 24900.0 nM 4.60