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Assay Detail

CHEMBL1943885

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

Binding
Inhibition of human recombinant BACE1 by FRET assay
10
Total Activities
10
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

Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design.
Hamada Y, Tagad HD, Nishimura Y, Ishiura S, Kiso Y.
Bioorg Med Chem Lett (2012) 22 : 1130 -1135
PubMed 22178553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.07 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439521 1 8.92
CHEMBL183546 1 8.41
CHEMBL255838 1 8.25
CHEMBL183494 1 8.09
CHEMBL453211 1 8.05
CHEMBL507541 1 8.00
CHEMBL501242 1 7.89
CHEMBL445281 1 7.82
CHEMBL448015 1 7.66
CHEMBL504917 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439521 IC50 = 1.2 nM 8.92
CHEMBL183546 IC50 = 3.9 nM 8.41
CHEMBL255838 IC50 = 5.6 nM 8.25
CHEMBL183494 IC50 = 8.2 nM 8.09
CHEMBL453211 IC50 = 9.0 nM 8.05
CHEMBL507541 IC50 = 10.0 nM 8.00
CHEMBL501242 IC50 = 13.0 nM 7.89
CHEMBL445281 IC50 = 15.0 nM 7.82
CHEMBL448015 IC50 = 22.0 nM 7.66
CHEMBL504917 IC50 = 24.0 nM 7.62