General
Preferred name
MAVATREP
Synonyms
JNJ-39439335 ()
P&D ID
PD058403
CAS
956274-94-5
Tags
available
drug candidate
probe
Drug indication
Musculoskeletal pain
Drug Status
investigational
Max Phase
Phase 1
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
2
No orthogonal probes found
Similar probes
0
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
Mavatrep (JNJ-39439335) is a TRPV1 antagonist that was designed for analgesic potential .
(GtoPdb)
MOA
Antagonist
(Chemical Probes.org)
DESCRIPTION
Mavatrep is an orally bioavailable, potent and selective TRPV1 antagonist with Ki value of 6.5 nM, which exhibits minimal effect on the enzymatic activity of CYP isoforms 3A4, 1A2, and 2D6. It antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM in a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels. It blocks the activation of hTRPV1 channels by Capsaicin and pH in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM respectively. It exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain in vivo. It was selected for clinical development for the treatment of pain. It was developed by Johnson & Johnson and now in clinic phase 1 with no progress.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
10
BOC Sciences Bioactive Compounds
ChEMBL Drugs
Chemical Probes.org
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
18
Molecular Weight
422.16
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
4
cLogP
6.65
TPSA
48.91
Fraction CSP3
0.16
Chiral centers
0.0
Largest ring
6.0
QED
0.39
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
transient receptor potential channel antagonist
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Target
TRP Channel
TRPV1
Solubility
DMSO:30mg/mL
Target class
Ion channel
Control
Cpd 28
Source data
