Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4009735

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

Binding
Inhibition of mouse glutaminyl cyclase assessed as reduction in conversion of H-Gln-AMC hydrobromide to pGlu-AMC preincubated with substrate for 10 mins followed by enzyme addition by pGAPase coupled fluorometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutaminyl-peptide cyclotransferase (CHEMBL4105900)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer's Agents Based on Rational Design.
Hoang VH, Tran PT, Cui M, Ngo VT, Ann J, Park J, Lee J, Choi K, Cho H, Kim H, Ha HJ, Hong HS, Choi S, Kim YH, Lee J.
J Med Chem (2017) 60 : 2573 -2590
PubMed 28234463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.79 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097599 1 7.90
CHEMBL566563 1 7.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097599 IC50 = 12.6 nM 7.90
CHEMBL566563 IC50 = 21.5 nM 7.67