General
Preferred name
PRX-07034
Synonyms
PRX-07034 HCL ()
PRX 07034 ()
PRX-07034 (hydrochloride) ()
PRX-07034 hydrochloride ()
N-[1-(5-chloro-2,3-dimethoxyphenyl)ethyl]-2-methanesulfonyl-5-(piperazin-1-yl)aniline ()
P&D ID
PD077628
CAS
903580-39-2
Tags
available
drug candidate
Drug indication
Obesity
Drug Status
investigational
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA PRX-07034 is a novel, highly selective, small-molecule antagonist of a specific G-protein coupled receptor (GPCR) known as 5-HT6 being developed for the treatment of obesity, Alzheimer's disease and cognitive impairment associated with schizophrenia.; ; PRX-07034 has also been shown to enhance cognitive function in preclinical animal models of memory impairment through a dual mechanism of action.It has an effect on both the acetylcholine and glutamate neurotransmitter systems in the brain, which makes it a potentially complementary therapy to cholinesterase inhibitors, a class of drugs approved for the treatment of Alzheimer's disease.;
DESCRIPTION PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility[1].
PRICE 62
DESCRIPTION PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist (??100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors.
DESCRIPTION Potent and selective CB1 receptor antagonist (Tocris Bioactive Compound Library)
DESCRIPTION PRX-07034 is a potent and selective 5-HT6 receptor antagonist. It was shown to improve cognition and memory in rats. (BOC Sciences Bioactive Compounds)
DESCRIPTION PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist (≥100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors. (TargetMol Bioactive Compound Library)
DESCRIPTION Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells (TargetMol Bioactive Compound Library)
Compound Sets
7
BOC Sciences Bioactive Compounds
prx-07034-cas-903580-39-2-item-283731
DrugBank
DB05993
DrugMAP
DM5TLAP
MedChem Express Bioactive Compound Library
HY-14559
ReFrame library
TargetMol Bioactive Compound Library
T8720
H025-0367C
Tocris Bioactive Compound Library
6748
External IDs
22
Properties
(calculated by RDKit )
Molecular Weight
453.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
3.34
TPSA
79.9
Fraction CSP3
0.43
Chiral centers
1.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
5-HT Receptor
5-HT6
Primary Target
5-HT6 Receptors
MOA
Antagonist
Pathway
GPCR/G protein
Neuronal Signaling
Neuroscience
Source data