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Assay Detail

CHEMBL3755067

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

Binding
Inhibition of recombinant human BACE-1 using M-2420 as substrate preincubated for 1 hr followed by substrate addition measured after 15 mins by FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-secretase 1 (CHEMBL4822)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.
Zha X, Lamba D, Zhang L, Lou Y, Xu C, Kang D, Chen L, Xu Y, Zhang L, De Simone A, Samez S, Pesaresi A, Stojan J, Lopez MG, Egea J, Andrisano V, Bartolini M.
J Med Chem (2016) 59 : 114 -131
PubMed 26632651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.29 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753957 1 6.72
CHEMBL3752926 1 6.37
CHEMBL3753360 1 6.21
CHEMBL3752467 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753957 IC50 = 190.0 nM 6.72
CHEMBL3752926 IC50 = 430.0 nM 6.37
CHEMBL3753360 IC50 = 620.0 nM 6.21
CHEMBL3752467 IC50 = 1350.0 nM 5.87