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Assay Detail

CHEMBL5136535

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

Binding
Inhibition of GCS in human A-375 cells using C6-ceramide and UDP-glucose as substrate preincubated for 30 mins followed by substrate addition measured after 20 hrs by UDP-Glo glucosylceramide synthase based luminometer analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-375
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ceramide glucosyltransferase (CHEMBL2063)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modified Benzofuran-carboxamide Compounds as Glucosylceramide Synthase Inhibitors for Treating Diseases.
Sabnis RW.
ACS Med Chem Lett (2022) 13 : 879 -880
PubMed 35707161 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 10.51 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5182897 1 10.70
CHEMBL5170109 1 10.68
CHEMBL5191157 1 10.64
CHEMBL5177098 1 10.36
CHEMBL5195638 1 10.36
CHEMBL5197108 1 10.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5182897 EC50 = 0.02 nM 10.70
CHEMBL5170109 EC50 = 0.021 nM 10.68
CHEMBL5191157 EC50 = 0.023 nM 10.64
CHEMBL5177098 EC50 = 0.044 nM 10.36
CHEMBL5195638 EC50 = 0.044 nM 10.36
CHEMBL5197108 EC50 = 0.047 nM 10.33