General
Preferred name
TERFENADINE
Synonyms
Seldane-d ()
(¡À)-Terfenadine ()
MDL-991 ()
(??)-Terfenadine ()
MDL-991(¡À)-Terfenadine ()
(±)-Terfenadine ()
Antihistamine ()
NSC-758627 ()
Seldane ()
Terfenor ()
Histafen 120 ()
Terfex ()
Triludan ()
NSC-665802 ()
Terfenor Fte ()
Triludan Fte ()
Histafen ()
Terfinax 60 ()
RMI 9918 ()
RMI-9918 ()
Terfinax 120 ()
P&D ID
PD000887
CAS
50679-08-8
Tags
prodrug
natural product
drug
available
Approved by
FDA
Drug Status
approved
withdrawn
Drug indication
Allergy
Antihistaminic
Max Phase
Phase 4
First approval
1985
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DESCRIPTION Due to adverse effects on cardiac function, terfenadine has largely been superseded by fexofenadine. Terfenadine was completely withdrawn in the US in 1998.
DESCRIPTION Due to adverse effects on cardiac function, terfenadine has largely been superseded by its carboxylic acid metabolite . Terfenadine was completely withdrawn in the US in 1998. (GtoPdb)
DESCRIPTION Non-sedating H1 histamine receptor antagonist (LOPAC library)
DESCRIPTION H1 antagonist. Also KV11.1 (hERG) and Kir6 (KATP) channel blocker (Tocriscreen Plus)
DESCRIPTION Potent CXCR4 antagonist (Tocris Bioactive Compound Library)
Cell lines
1
Organisms
3
Compound Sets
29
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
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Ki Database
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Plus
VGSC-DB
Withdrawn 2.0
External IDs
34
Properties
(calculated by RDKit )
Molecular Weight
471.31
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
3
cLogP
6.45
TPSA
43.7
Fraction CSP3
0.44
Chiral centers
1.0
Largest ring
6.0
QED
0.4
QED
0.4
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Selectivity
H1
Pathway
GPCR/G protein
Membrane Transporter/Ion Channel
Neuroscience
Angiogenesis
JAK/STAT Signaling
Tyrosine Kinase/Adaptors
Apoptosis
Immunology/Inflammation
Neuronal Signaling
Target
HT
mAChR
Potassium Channel
HERG
Caspase
Histamine Receptor
Na+/Ca2+ Exchanger
Calcium Channel,Caspase,Histamine Receptor,NCX,Potassium Channel
Primary Target
Histamine H1 Receptors
MOA
Antagonist
ATC
R06AX12
Toxicity type
cardiovascular
Therapeutic Class
Antihistamines
VGSC Target
Nav1.5
Source data