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Probe
AZD3293 is in
the process of SERP review.
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commentary.
Information
BACE1
BACE2
Inhibitor
up to 100 nM
In Vitro Validations
Uniprot ID: P56817
Target Class:
Enzyme
Target SubClass: Peptidase
Potency: Ki
Potency Value: 0.4 nM
Potency Assay: TR-FRET assays
PDB ID for probe-target interaction (3D structure):
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AZD3293 is a highly potent inhibitor of both BACE1 (IC50: 0.6 nM in vitro) and BACE2 AM-6494 (IC50: 0.9 nM in vitro) with high selectivity over hCathepsin D (IC50: 16100 nM) and hERG (IC50: 4700nM). A not further described panel of more than 350 in vitro assays covering receptors, ion channels, transporters, kinases and other enzymes suggests a 1,000-fold selectivity against BACE1/2. In vivo studies in mice, guinea pigs, dogs and humans (AMARANTH (NCT02245737)) have been performed.
Other probes with selectivity against BACE1 over BACE2 like AM-6494 are already available and should be considered if this selectivity is desired.
