General
Preferred name
darigabat
Synonyms
PF-06372865 ()
CVL-865 ()
Cvl-865 ()
P&D ID
PD076499
CAS
1614245-70-3
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
Drug indication
reflex epilepsy
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 PF-06372865 is an orally active, GABAA receptor positive allosteric modulator, that selectively targets GABAA receptors containing α2/3/5 subunits over receptors containing α1 subunits . The α1 subunit is associated with the (undesirable) sedative effects of benzodiazepine drugs, whilst the α2/3 subunits contribute to their anxiolytic and analgesic activities and the α5 subunit to effects on memory function. The chemical structure of PF-06372865 is claimed as 'Example 4' in patent WO2014091368 . Pfizer are developing PF-06372865 for clinical potential in the treatment of chronic pain, generalized anxiety disorder and epilepsy.
DESCRIPTION PF-06372865 is an orally active, ¦Á2/¦Á3/¦Á5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing ¦Á1/¦Á2/¦Á3/¦Á5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for ¦Á2, ¦Á1 PAM, ¦Á2 PAM, respectively), with low affinity for ¦Á4/¦Á6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy[1].
PRICE 32
DESCRIPTION Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for ??2, ??1 PAM, and ??2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.
DESCRIPTION Darigabat (PF-06372865) is an orally active, GABAA receptor positive allosteric modulator, that selectively targets GABAA receptors containing α2/3/5 subunits over receptors containing α1 subunits . The α1 subunit is associated with the (undesirable) sedative effects of benzodiazepine drugs, whilst the α2/3 subunits contribute to their anxiolytic and analgesic activities and the α5 subunit to effects on memory function. The chemical structure of this compound is claimed as 'Example 4' in patent WO2014091368 . Pfizer are developing PF-06372865 for clinical potential in the treatment of chronic pain and photosensitive epilepsy, but have terminated development in generalized anxiety disorder. (GtoPdb)
Compound Sets
7
ChEMBL Drugs
CHEMBL3647536
DrugBank
DB18966
EUbOPEN Chemogenomics Library
EUB0002019
Guide to Pharmacology
9798
MedChem Express Bioactive Compound Library
HY-120874
ReFrame library
VGSC-DB
NA3322
External IDs
14
Properties
(calculated by RDKit )
Molecular Weight
440.13
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
0
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
4
cLogP
4.12
TPSA
86.97
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.45
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
GABA Receptor
VGSC Target
Nav1.5
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Recommended Cell Concentration
1 uM
Source data