General
Preferred name
intepirdine
Synonyms
Intepirdine ()
SB-742457 ()
RVT-101 ()
SB 742457 ()
GSK-742457 ()
SB 742457 hydrochloride ()
GSK 742457 ()
SB742457 ()
SB-742457 ()
INTEPIRDINA ()
GSK742457 ()
P&D ID
PD010528
CAS
607742-69-8
607742-55-2
Tags
available
drug candidate
Drug indication
Alzheimer disease
Dementia
Drug Status
investigational
Max Phase
3.0
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 Intepirdine (RVT-101) is a 5-HT6 receptor antagonist (called SB-742457 in this article). Developed by Axovant Science Ltd.
Phase 3 clinical trial results for RVT-101 are eagerly awaited given the reported failures of competitors' 5-HT6 receptor antagonists in Alzheimer's disease trials (e.g. Lundbeck's , and Pfizer's PF-05212377). (GtoPdb)
DESCRIPTION Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.
PRICE 41
DESCRIPTION Intepirdine (GSK-742457) is a highly selective 5-HT6 receptor antagonist, used in trials studying the treatment of Alzheimer's Disease. (TargetMol Bioactive Compound Library)
DESCRIPTION SB 742457 hydrochloride is a selective 5-HT6 antagonist with >100-fold selectivity over other receptors. It is a potential agent added to stabilize donepezil treatment in subjects with mild-to-moderate Alzheimer's disease. (BOC Sciences Bioactive Compounds)
Compound Sets
16
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
External IDs
37
Properties
(calculated by RDKit )
Molecular Weight
353.12
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
4
Aromatic Ring Count
3
cLogP
2.48
TPSA
62.3
Fraction CSP3
0.21
Chiral centers
0.0
Largest ring
6.0
QED
0.78
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
5-HT Receptor
5-HT6
HTR6
5-HT6 antagonist
MOA
serotonin receptor antagonist
Pathway
GPCR/G protein
Neuronal Signaling
Neuroscience
Recommended Cell Concentration
100 nM
Source data