General
Preferred name
DOFETILIDE
Synonyms
UK 68789 ()
UK-68798 ()
Tikosyn ()
UK-68,798 ()
Dofetilida ()
Dofetilide-d4 ()
P&D ID
PD003019
CAS
115256-11-6
1189700-56-8
Tags
available
drug
Approved by
FDA
First approval
1999
Drug indication
Sinus rhythm disorder
cardiac arrhythmia
Drug Status
approved
withdrawn
investigational
Max Phase
4.0
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 Dofetilide blocks potassium voltage-gated channels (HERGs). (GtoPdb)
DESCRIPTION Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease[1][2].
PRICE 59
DESCRIPTION K2P2.1 (TREK-1) and K2P10.1 (TREK-2) activator (Tocris Bioactive Compound Library)
DESCRIPTION KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr) (Tocriscreen Plus)
DESCRIPTION Dofetilide is a class III antiarrhythmic drug used for the maintenance of normal sinus rhythm and cardioversion in cases of atrial fibrillation and atrial flutter. Dofetilide blocks only IKr with no relevant block of the other repolarizing potassium currents. (Enamine Bioactive Compounds)
DESCRIPTION Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
36
AdooQ Bioactive Compound Library
A10328
Axon Medchem Screening Library
2103
Cayman Chemical Bioactives
15045
26451
ChEMBL Approved Drugs
CHEMBL473
ChEMBL Drugs
CHEMBL473
Concise Guide to Pharmacology 2017/18
2604
Concise Guide to Pharmacology 2019/20
2604
Concise Guide to Pharmacology 2021/22
2604
Concise Guide to Pharmacology 2023/24
2604
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB00204
DrugBank Approved Drugs
DB00204
DrugCentral
942
DrugCentral Approved Drugs
942
DrugMAP
DMPN1TW
DrugMAP Approved Drugs
DMPN1TW
DrugMatrix
Enamine Bioactive Compounds
EBC-11239
EU-OPENSCREEN Bioactive Compound Library
EOS101379
Guide to Pharmacology
2604
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL473
Mcule NIBR MoA Box Subset
MCULE-1740129117
MedChem Express Bioactive Compound Library
HY-B0232
NCATS Inxight Approved Drugs
R4Z9X1N2ND
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
Dofetilide(Tikosyn)
TargetMol Bioactive Compound Library
T6476
Tocris Bioactive Compound Library
3757
Tocriscreen Plus
3757
VGSC-DB
NA0096
NA0097
NA0098
Withdrawn 2.0
w64
External IDs
44
Properties
(calculated by RDKit )
Molecular Weight
441.14
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
11
Ring Count
2
Aromatic Ring Count
2
cLogP
1.98
TPSA
104.81
Fraction CSP3
0.37
Chiral centers
0.0
Largest ring
6.0
QED
0.55
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Target
Potassium Channel
KCNH1, KCNH2, KCNJ12, KCNK2
Kv11.1 channel blocker
Primary Target
Voltage-gated Potassium (KV) Channels
MOA
Blocker
K(V)11.1 (erg1) Channel Blockers
potassium channel blocker
Member status
member
ATC
C01BD04
Toxicity type
cardiovascular
Therapeutic Class
Antiarrhythmic Agents
VGSC Target
Nav1.5
Pathway
Membrane Transporter/Ion Channel
Source data