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Assay Detail

CHEMBL929600

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

Binding
Inhibition of human recombinant BACE1 by FRET assay
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel non-peptidic and small-sized BACE1 inhibitors.
Hamada Y, Ohta H, Miyamoto N, Yamaguchi R, Yamani A, Hidaka K, Kimura T, Saito K, Hayashi Y, Ishiura S, Kiso Y.
Bioorg Med Chem Lett (2008) 18 : 1643 -1647
PubMed 18261904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.67 8.92
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439521 1 8.92
CHEMBL183546 1 8.41
CHEMBL381826 1 8.32
CHEMBL183494 1 8.09
CHEMBL378225 1 7.82
CHEMBL42908 1 7.52
CHEMBL400043 1 7.30
CHEMBL399840 1 7.02
CHEMBL399839 1 6.85
CHEMBL253865 1 6.44
CHEMBL413920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439521 IC50 = 1.2 nM 8.92
CHEMBL183546 IC50 = 3.9 nM 8.41
CHEMBL381826 IC50 = 4.8 nM 8.32
CHEMBL183494 IC50 = 8.2 nM 8.09
CHEMBL378225 IC50 = 15.0 nM 7.82
CHEMBL42908 IC50 = 30.0 nM 7.52
CHEMBL400043 IC50 = 50.0 nM 7.30
CHEMBL399840 IC50 = 96.0 nM 7.02
CHEMBL399839 IC50 = 140.0 nM 6.85
CHEMBL253865 IC50 = 360.0 nM 6.44
CHEMBL413920 Activity - -