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Assay Detail

CHEMBL5525872

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

Binding
Positive allosteric modulation of GCase in human Fibroblast cells using GBA1-FQ2 as substrate preincubated for 24 hrs followed by substrate addition and measured after 3 hrs by Hoechst 33342 staining based imaging analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysosomal acid glucosylceramidase (CHEMBL2179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β-Glucocerebrosidase.
Palmer N, Agnew C, Benn C, Buffham WJ, Castro JN, Chessari G, Clark M, Cons BD, Coyle JE, Dawson LA, Hamlett CCF, Hodson C, Holding F, Johnson CN, Liebeschuetz JW, Mahajan P, McCarthy JM, Murray CW, O'Reilly M, Peakman T, Price A, Rapti M, Reeks J, Schöpf P, St-Denis JD, Valenzano C, Wallis NG, Walser R, Weir H, Wilsher NE, Woodhead A, Bento CF, Tisi D.
J Med Chem (2024) 67 : 11168 -11181
PubMed 38932616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 4.77 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5560927 1 5.05
CHEMBL5562071 1 5.05
CHEMBL153479 AMBROXOL 3.0 1 4.53
CHEMBL5567650 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5560927 EC50 = 8900.0 nM 5.05
CHEMBL5562071 EC50 = 9000.0 nM 5.05
CHEMBL153479 AMBROXOL EC50 = 29400.0 nM 4.53
CHEMBL5567650 EC50 = 37100.0 nM 4.43