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Assay Detail

CHEMBL2032679

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

Binding
Competitive inhibition of wild type human glucocerebrosidase using 4-methylumbelliferyl beta-D-glucopyranoside as substrate after 15 mins by Dixon and Line-Weaver Burk plot analysis at pH 5
9
Total Activities
9
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

Rapid assembly of a library of lipophilic iminosugars via the thiol-ene reaction yields promising pharmacological chaperones for the treatment of Gaucher disease.
Goddard-Borger ED, Tropak MB, Yonekawa S, Tysoe C, Mahuran DJ, Withers SG.
J Med Chem (2012) 55 : 2737 -2745
PubMed 22360565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.34 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2029773 1 9.40
CHEMBL2029772 1 8.74
CHEMBL2029780 1 8.52
CHEMBL2029778 1 8.40
CHEMBL2029776 1 8.36
CHEMBL2029777 1 8.22
CHEMBL2029782 1 7.92
CHEMBL2029771 1 7.75
CHEMBL2029779 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2029773 Ki = 0.4 nM 9.40
CHEMBL2029772 Ki = 1.8 nM 8.74
CHEMBL2029780 Ki = 3.0 nM 8.52
CHEMBL2029778 Ki = 4.0 nM 8.40
CHEMBL2029776 Ki = 4.4 nM 8.36
CHEMBL2029777 Ki = 6.0 nM 8.22
CHEMBL2029782 Ki = 12.0 nM 7.92
CHEMBL2029771 Ki = 18.0 nM 7.75
CHEMBL2029779 Ki = 19.0 nM 7.72