General
Preferred name
VU0152100
Synonyms
VU 152100 ()
ML108 ()
VU152100 ()
VU 0152100 ()
P&D ID
PD010246
CAS
409351-28-6
Tags
probe
drug candidate
available
Drug indication
Discovery agent
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
5
No orthogonal probes found
Similar probes
2
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
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia[1][2].
PRICE
95
DESCRIPTION
VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ?? 93 nM).
DESCRIPTION
To identify small molecule positive allosteric modulators and/or allosteric agonists of the M4 muscarinic acetylcholine receptor that are cell permeable, possess submicromolar potency and show greater than 10-fold selectivity over the other mAChRs (M1, M2, M3 and M5) employing a functional HTS approach.
(MLP Probes)
DESCRIPTION
High affinity, selective mGlu1 antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Positive allosteric modulator of M4 receptors
(Tocriscreen Plus)
DESCRIPTION
VU0152100 is a selective and positive allosteric modulators of M4 receptor. It has shown a potent positive allosteric modulators that increase the response of the M4 receptor to the endogenous agonist ACh in in vitro study. And it has been revealed to enhance receptor activation by increasing the affinity of M4 for acetylcholine.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
VU0152100 is an effective and selective allosteric potentiator of M4 mAChR (EC50: 380 ± 93 nM).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
16
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
Guide to Pharmacology
MedChem Express Bioactive Compound Library
MLP Probes
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
17
Molecular Weight
341.12
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
3
cLogP
3.43
TPSA
77.24
Fraction CSP3
0.22
Chiral centers
0.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Antitarget
M1, M2, M3, M5, PanLabs
Target
M4
M4 mAChR
mAChR
CHRM4
PAM of M4 mAChR
Primary Target
M4 Receptors
MOA
Modulator
acetylcholine receptor allosteric modulator
Pathway
Neuroscience
GPCR/G protein
Neuronal Signaling
Source data
