General
Preferred name
SENICAPOC
Synonyms
ICA-17043 ()
Senicapoc (ICA-17043) ()
PF-05416266 ()
P&D ID
PD012234
CAS
289656-45-7
Tags
available
drug candidate
Drug indication
severe acute respiratory syndrome
Alzheimer disease
Constitutional neutropenia
Drug Status
investigational
Max Phase
3.0
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 Senicapoc has activity as a KCa3.1 channel inhibitor. [18]F-labelled senicapoc derivatives have been used as positron emission tomography tracers to visualise KCa3.1 channels in vivo . A BODIPY-conjugated (fluorescent) senicapoc probe that occupies space in the channel pore is also reported . (GtoPdb)
DESCRIPTION Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM[1].
PRICE 37
DESCRIPTION Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel that ameliorates RBC dehydration in the SAD mouse. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ?? 2 nM (CLT IC50 = 100 ?? 12 nM) and inhibits RBC dehydration with an IC50 of 30 ?? 20 nM. Senicapoc is used in the treatment of Sickle Cell Disease and Sickle Cell Anemia.
DESCRIPTION Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel that ameliorates RBC dehydration in the SAD mouse. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibits RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is used in the treatment of Sickle Cell Disease and Sickle Cell Anemia. (TargetMol Bioactive Compound Library)
Compound Sets
19
AdooQ Bioactive Compound Library
A11568
Cayman Chemical Bioactives
29679
ChEMBL Drugs
CHEMBL405821
Concise Guide to Pharmacology 2019/20
2331
Concise Guide to Pharmacology 2021/22
2331
Concise Guide to Pharmacology 2023/24
2331
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB06280
DrugMAP
DMRFY7I
EU-OPENSCREEN Bioactive Compound Library
EOS101164
Guide to Pharmacology
2331
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL405821
MedChem Express Bioactive Compound Library
HY-50694
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
senicapoc-ica-17043
TargetMol Bioactive Compound Library
T3528
VGSC-DB
NA0119
NA0120
NA0121
NA0122
NA0123
NA0124
External IDs
25
Properties
(calculated by RDKit )
Molecular Weight
323.11
Hydrogen Bond Acceptors
1
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
3
cLogP
3.78
TPSA
43.09
Fraction CSP3
0.05
Chiral centers
0.0
Largest ring
6.0
QED
0.73
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Gardos channel
Potassium Channel
KCNN4
MOA
Potassium Channel inhibitor
Intermediate Conductance K(Ca) 3.1 (IKCa1
Gardos channel, SK41, IK1) Channel Blockers
intermediate conductance potassium channel blocker
Member status
member
VGSC Target
Nav1.1
Nav1.2
Nav1.3
Nav1.4
Nav1.6
Nav1.7
Pathway
Membrane Transporter/Ion Channel
Source data