Atabecestat (JNJ-54861911, JNJ54861911) is a novel potent, oral beta-secretase (BACE) inhibitor for treatment of Alzheimer's Disease.

AZD3293 is a potent and selective orally active, brain-permeable BACE1 inhibitor,currently in development as a potential treatment for early Alzheimer’s disease.

AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

beta-secretase inhibitor.

Elenbecestat (E2609) is a novel potent, oral BACE1 inhibitor for treatment of Alzheimer's disease..

LY2811376 is the first orally available non-peptidicβ-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM.

LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease.

MK-8931 is a BACE1 inhibitor. MK-8931 binds significantly to β-secretase.

Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 μM.

Cassiaside is a naphthopyrone glucoside, shows mixed-type inhibition against BACE1 (IC50=4.45 μM; Ki=9.85 μM). Cassiaside possesses potential anti- Alzheimer's disease (AD) activity.

β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total Aβ and IC50=2.5 μM for Aβ1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.

BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay.

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.

β-Secretase Inhibitor I is an extremely potent β-secretase inhibitor with reduced cardiovascular and liver toxicity.

JNJ-67569762 is a tetrahydropyridine-based BACE1 inhibitor targeting the S3 pocket with IC50 of 2.7 nM and shows 71-fold selectivity over BACE2.

β-Secretase Inhibitor III is an extremely selective BACE1 inhibitor (Ki = 0.13 nM).

BACE1-IN-6 is a BACE1 inhibitor with an IC50 value of 1.5 nM.

BACE1-IN-7-18F can be developed as a PET tracer for in vivo imaging of BACE1. The unlabeled BACE1-IN-7 is a potent BACE1 inhibitor (IC50=13.2 nM).