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Assay Detail

CHEMBL5226007

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

Binding
Inhibition of GCS in human iPSC derived neurons assessed as reduction in brain GlcCer levels
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ceramide glucosyltransferase (CHEMBL2063)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME.
ACS Med Chem Lett (2023) 14 : 146 -155
PubMed 36793422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 1 - -
IC50 1 8.77 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5275403 2 8.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5275403 IC50 = 1.7 nM 8.77
CHEMBL5275403 Inhibition - % -