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Assay Detail

CHEMBL2388915

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

Binding
Inhibition of recombinant human BACE1 extracellular domain expressed in baculovirus using Q-C(HS03)-lle-Asp-Leu-Ala-Val-Leu-Asp-HN-CH2-CH2-Mca as substrate incubated for 1 hr measured every 1 min for 15 mins by fluorescence assay
8
Total Activities
8
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

Dihydrooxazines As Inhibitors of BACE-1 or BACE-2.
Rosse G.
ACS Med Chem Lett (2013) 4 : 433 -434
PubMed 24900690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.42 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386720 1 7.92
CHEMBL2386719 1 7.92
CHEMBL2386724 1 7.75
CHEMBL2386726 1 7.72
CHEMBL2386721 1 7.54
CHEMBL2386723 1 7.46
CHEMBL2386722 1 7.00
CHEMBL2386725 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386720 IC50 = 12.0 nM 7.92
CHEMBL2386719 IC50 = 12.0 nM 7.92
CHEMBL2386724 IC50 = 18.0 nM 7.75
CHEMBL2386726 IC50 = 19.0 nM 7.72
CHEMBL2386721 IC50 = 29.0 nM 7.54
CHEMBL2386723 IC50 = 35.0 nM 7.46
CHEMBL2386722 IC50 = 100.0 nM 7.00
CHEMBL2386725 IC50 = 830.0 nM 6.08