General
Preferred name
VU 0238429
Synonyms
ML129 ()
SCR-1481B1 ()
VU0238429 ()
M5 PAM ()
P&D ID
PD016004
CAS
1160247-92-6
Tags
available
probe
drug candidate
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
3
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
To identify small molecule positive allosteric modulators (PAMs) and/or allosteric agonists of the M1 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 M4) employing a functional HTS approach.
(MLP Probes)
DESCRIPTION
Selective positive allosteric modulator of M5 receptors
(Tocriscreen Plus)
DESCRIPTION
Potent and selective H4 antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Selective positive allosteric modulator of M5 receptors
(Tocriscreen Total)
DESCRIPTION
VU 0238429 is a selective positive allosteric modulator of M5 muscarinic acetylcholine receptor (EC50 = 1.16, >30 and >30 μM at M5, M1 and M3 receptors, respectively) with no activity at M2 and M4 receptors.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
16
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
Guide to Pharmacology
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
MLP Probes
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
17
Molecular Weight
351.07
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
0
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
2
cLogP
3.32
TPSA
55.84
Fraction CSP3
0.18
Chiral centers
0.0
Largest ring
6.0
QED
0.79
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Antitarget
M1, M2, M3, M4
Target
mAChR 5 (M5)
M5 mAChR
CHRM5
M5 PAM
mAChR
AChR
Pathway
Neuroscience
GPCR/G protein
Neuronal Signaling
Primary Target
M5 Receptors
MOA
Modulator
M5 positive allosteric modulator
acetylcholine receptor allosteric modulator
Member status
member
Source data
