General
Preferred name
Azetukalner
Synonyms
XEN1101 ()
KCNQ2/3 activator-1 ()
ENCUKALNER ()
XEN-1101 ()
P&D ID
PD164779
CAS
1009344-33-5
Tags
drug candidate
available
Drug Status
investigational
Max Phase
3.0
Drug indication
Major depressive disorder
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 Azetukalner (XEN1101) is a selective and orally active Kv7.2/Kv7.3 potassium channel opener with an EC50 of 27 nM. Azetukalner is approximately 4-fold more selective for Kv7.2/7.3 over Kv7.3/7.5 (EC50 of 94 nM) and Kv7.4 (EC50 of 113 nM) channels. Azetukalner exhibits a selectivity >100-fold for Kv7 channels over other ion channels and receptors. Azetukalner can be used for the study of focal epilepsy[1][2].
PRICE 70
DESCRIPTION Encukalner (XEN1101) is a clinical stage voltage-gated potassium channel (Kv7) activator , that was developed as a potential anti-epileptic drug, or for the treatment of major depressive disorder. It activates Kv7.2 and Kv7.3 channel subtypes. (GtoPdb)
DESCRIPTION KCNQ2/3 activator-1 is a Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator, details of which are from Compound A of Patent WO2021113757A1. (TargetMol Bioactive Compound Library)
Compound Sets
4
ChEMBL Drugs
CHEMBL5095264
Guide to Pharmacology
12650
MedChem Express Bioactive Compound Library
HY-139791
TargetMol Bioactive Compound Library
T9400
External IDs
10
Properties
(calculated by RDKit )
Molecular Weight
368.23
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
2
cLogP
5.38
TPSA
32.34
Fraction CSP3
0.43
Chiral centers
0.0
Largest ring
6.0
QED
0.79
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Kv7.2
Potassium Channel
Pathway
Membrane Transporter/Ion Channel
Source data