General
Preferred name
meclinertant
Synonyms
CHEMBL506981 ()
SR-48692 ()
REMINERTANT ()
SR 48692 ()
[3H]meclinertant ()
SR48692 ()
[3H]meclinertant ()
P&D ID
PD016831
CAS
146362-70-1
Tags
available
probe
drug candidate
Drug indication
Discovery agent
small cell lung carcinoma
Inflammatory bowel disease
Drug Status
investigational
Max Phase
3.0
Probe info
Probe type
P&D approved
calculated probe
Probe selectivity
protein-selective
Probe sources
High-quality chemical probes
Probe Miner (suitable probes)
Tool Compound Set
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 843
DESCRIPTION Highly selective M1 antagonist (Tocris Bioactive Compound Library)
DESCRIPTION Meclinertant, a chloroquinolin derivative, has been found to be a Neurotensin receptor antagonist that could be probably effective against schizophrenia and some sorts of drug addiction at some extent. It has been already discontinued by sanofi-aventis for Small cell lung cancer. IC50: 15.3 and 20.4 nM for NTS1 and NTS2 respectively. (BOC Sciences Bioactive Compounds)
DESCRIPTION Meclinertant (SR 48692) is a neurotensin receptor-1 (NT1) antagonist that blocks neurotensin-induced excitation and can be used to study neurological disorders. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
25
Axon Medchem Screening Library
1164
BOC Sciences Bioactive Compounds
meclinertant-cas-146362-70-1-item-424305
Cayman Chemical Bioactives
20124
ChEMBL Drugs
CHEMBL506981
Concise Guide to Pharmacology 2017/18
1582
1583
Concise Guide to Pharmacology 2019/20
1582
1583
Concise Guide to Pharmacology 2021/22
1582
1583
Concise Guide to Pharmacology 2023/24
1582
1583
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB06455
DrugMAP
DMBIO6E
DMEX6GT
DrugMatrix
EUbOPEN Chemogenomics Library
EUB0000385
Guide to Pharmacology
1582
1583
High-quality chemical probes
PD016831
Ki Database
SR 48692
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL506981
Novartis Chemogenetic Library (NIBR MoA Box)
Probe Miner (suitable probes)
P30989/859769
ReFrame library
TargetMol Bioactive Compound Library
T16034
Tocris Bioactive Compound Library
3721
Tool Compound Set
ZINC Tool Compounds
ZINC000001482927
External IDs
36
Properties
(calculated by RDKit )
Molecular Weight
586.2
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
8
Aromatic Ring Count
4
cLogP
5.77
TPSA
115.57
Fraction CSP3
0.38
Chiral centers
0.0
Largest ring
6.0
QED
0.28
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Neurotensin receptor 1
NTR1
NTSR1, NTSR2
NT1 antagonist
Primary Target
Neurotensin Receptors
MOA
Antagonist
Carboxypeptidase A Inhibitors
Neurotensin NTS1 (NT1) Receptor Antagonists
neurotensin receptor antagonist
Member status
member
Therapeutic Class
Anticancer Agents
Pathway
GPCR/G protein
Recommended Cell Concentration
10 uM
Source data