General
Preferred name
GEFAPIXANT
Synonyms
AF219 ()
MK-7264 citrate ()
AF-219 citrate ()
RO4926219 citrate ()
AF219 citrate ()
MK7264 citrate ()
RO 4926219 citrate ()
RO 4926219 ()
AF 219 ()
AF-219 ()
Gefapixant (citrate) ()
MK-7264 ()
MK-7264 (citrate) ()
AF-219 (citrate) ()
AF-219, MK-7264, R1646,RG-1646,RO 4926219 ()
GEFAPIXANT CITRATE ()
R-1646 ()
RG-1646 ()
RG1646 ()
RO4926219 ()
R1646 ()
Ro-4926219 ()
AF-219 CITRATE ()
MK-7264 CITRATE ()
MK7264 CITRATE ()
MK7264 ()
Lyfnua ()
P&D ID
PD057987
CAS
1015787-98-0
2310299-91-1
Tags
available
drug
Approved by
PMDA
First approval
2022
2023
Drug indication
Cough
Overactive bladder
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
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
AF-219 is a P2X3 receptor antagonist.
DESCRIPTION
Gefapixant (MK‐7264, and formerly AF-219) is a P2X3 and P2X2/3 receptor antagonist. Experimental results have shown that gefapixant acts as a reversible allosteric antagonist, that exhibits preferential activity at closed channels.
Studies in rodent models have provided evidence that supports investigation of gefapixant as a novel treatment for chronic sensitisation conditions . (GtoPdb)
Studies in rodent models have provided evidence that supports investigation of gefapixant as a novel treatment for chronic sensitisation conditions . (GtoPdb)
PRICE
62
DESCRIPTION
Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
DESCRIPTION
Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3].
PRICE
81
DESCRIPTION
Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist.
(Enamine Bioactive Compounds)
DESCRIPTION
Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2/3. It can be used to study chronic cough.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
22
AdooQ Bioactive Compound Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
30
Molecular Weight
353.12
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
3
Rotatable Bonds
5
Ring Count
2
Aromatic Ring Count
2
cLogP
1.21
TPSA
156.44
Fraction CSP3
0.29
Chiral centers
0.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
P2X3
P2X Receptor
MOA
P2 Receptor
purinergic receptor antagonist
Pathway
Neuroscience
Membrane Transporter/Ion Channel
Source data
