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Assay Detail

CHEMBL2168216

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

Binding
Binding affinity to recombinant imiglucerase using 4-methylumbelliferyl-beta-D-glucopyranoside as substrate preincubated for 30 mins before substrate addition 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
Ki 10 6.61 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164231 1 9.00
CHEMBL2164227 1 7.50
CHEMBL2164230 1 7.28
CHEMBL2164232 1 6.89
CHEMBL2164229 1 6.55
CHEMBL408500 1 6.52
CHEMBL2164233 1 6.09
CHEMBL2164228 1 5.80
CHEMBL2163840 1 5.72
CHEMBL2163841 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164231 Ki = 1.0 nM 9.00
CHEMBL2164227 Ki = 32.0 nM 7.50
CHEMBL2164230 Ki = 53.0 nM 7.28
CHEMBL2164232 Ki = 130.0 nM 6.89
CHEMBL2164229 Ki = 280.0 nM 6.55
CHEMBL408500 Ki = 300.0 nM 6.52
CHEMBL2164233 Ki = 820.0 nM 6.09
CHEMBL2164228 Ki = 1580.0 nM 5.80
CHEMBL2163840 Ki = 1900.0 nM 5.72
CHEMBL2163841 Ki = 17900.0 nM 4.75