General
Preferred name
Lorediplon
Synonyms
Gf-015535-00 ()
P&D ID
PD012259
CAS
917393-39-6
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.;Target: GABA;Lorediplon is a drug for the treatment of insomnia, has been successfully completed with a best-in-class efficacy profile in terms of maintaining sleep and sleep quality, Lorediplon targets GABAA. [1] Lorediplon demonstrates a minimum of 10-fold and 6-fold increase in potency (respectively) in the spontaneous motor activation studies. At concentrations of 1.2mg/kg, Lorediplon demonstrates a 57%increased effect on Slow Wave Sleep (SWS), when compared with a placebo.[2]
PRICE 32
DESCRIPTION Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the ??1-subunit, associated with promoting sleep.
DESCRIPTION Lorediplon is a hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit. It is a novel nonbenzodiazepine of the pyrazolopyrimidine family. It is a drug for the treatment of insomnia. It demonstrated a dose-dependent improvement in sleep. It has been successfully completed with a best-in-class efficacy profile in terms of maintaining sleep and sleep quality. It demonstrates a minimum of 10-fold and 6-fold increase in potency in the spontaneous motor activation studies. It was developed by Ferrer and has been in Cilinic Phase 2. (BOC Sciences Bioactive Compounds)
DESCRIPTION Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep. (TargetMol Bioactive Compound Library)
Compound Sets
8
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
MedChem Express Bioactive Compound Library
ReFrame library
TargetMol Bioactive Compound Library
External IDs
16
Properties
(calculated by RDKit )
Molecular Weight
394.09
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
0
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
4
cLogP
3.81
TPSA
67.57
Fraction CSP3
0.1
Chiral centers
0.0
Largest ring
6.0
QED
0.49
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
GABA Receptor
GABAA
GABRA1
MOA
GABA Receptor modulator
Pathway
Membrane Transporter/Ion Channel
Neuroscience
Neuronal Signaling
Solubility
10 mM in DMSO
Source data