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Assay Detail

CHEMBL3269334

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

Binding
Inhibition of recombinant soluble human BACE1 catalytic domain using QSY7-EISEVNLDAEFC-Europium-amide as substrate preincubated for 30 mins followed by substrate addition measured after 1.5 hrs by time-resolved FRET assay
3
Total Activities
3
Compounds Tested
2
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

The evolution of amidine-based brain penetrant BACE1 inhibitors.
Oehlrich D, Prokopcova H, Gijsen HJ.
Bioorg Med Chem Lett (2014) 24 : 2033 -2045
PubMed 24704031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.54 9.00
Ki 1 7.57 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261078 1 9.00
CHEMBL3261079 1 8.08
CHEMBL3261056 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261078 IC50 = 1.0 nM 9.00
CHEMBL3261079 IC50 = 8.4 nM 8.08
CHEMBL3261056 Ki = 27.2 nM 7.57