General
Preferred name
LY-2811376
Synonyms
LY2811376 ()
LY 2811376 ()
Ly2811376 ()
J3.079.793K ()
P&D ID
PD010991
CAS
1194044-20-6
Tags
available
drug candidate
Drug indication
Alzheimer disease
Drug Status
investigational
Max Phase
1.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
LY2811376 is the first orally available non-peptidic ¦Â-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease A¦Â secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
PRICE
150
DESCRIPTION
LY2811376, an orally available non-peptidic ??-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease A?? secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.
DESCRIPTION
LY2811376 is a non-peptidic BACE1 inhibitor for Alzheimer's Disease. Aβ reductions in lumbar CSF were measured after oral dosing in humans but development was halted because of toxicology findings but these may not be related to BACE1 inhibition.
(GtoPdb)
DESCRIPTION
LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
15
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
320.09
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
3
Aromatic Ring Count
2
cLogP
3.3
TPSA
61.66
Fraction CSP3
0.27
Chiral centers
1.0
Largest ring
6.0
QED
0.89
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Aβ
BACE1
Beta-secretase
BACE 1 inhibitor
BACE,Beta Amyloid
Member status
member
MOA
BACE1 gene inhibitor
beta-secretase inhibitor
Pathway
Neuronal Signaling
Neuroscience
Source data
