General
Preferred name
GSK-256066
Synonyms
GSK 256066 Trifluoroacetate ()
O66 ()
GSK256066 ()
GSK256066 (Trifluoroacetate) ()
GSK256066 2,2,2-trifluoroacetic acid ()
P&D ID
PD010917
CAS
13122-87-7
801312-28-7
1415560-64-3
Tags
available
drug candidate
probe
Drug indication
Chronic obstructive pulmonary disease
Asthma
Drug Status
investigational
Max Phase
2.0
Probe info
Probe type
calculated probe
experimental probe
Probe targets
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 GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease[1].
DESCRIPTION GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease[1].
PRICE 131
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. (BOC Sciences Bioactive Compounds)
DESCRIPTION GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. (BOC Sciences Bioactive Compounds)
DESCRIPTION GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380, 000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
15
Cayman Chemical Bioactives
ChEMBL Drugs
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
High-quality chemical probes
MedChem Express Bioactive Compound Library
Probe Miner (suitable probes)
ReFrame library
TargetMol Bioactive Compound Library
External IDs
39
Properties
(calculated by RDKit )
Molecular Weight
518.16
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
4
cLogP
3.93
TPSA
131.69
Fraction CSP3
0.15
Chiral centers
0.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
PDE4B
phosphodiesterase
PDE4A
Phosphodiesterase (PDE)
MOA
phosphodiesterase inhibitor
Orthogonal probe
R(-)Rolipram
Pathway
Metabolism
Metabolic Enzyme/Protease
Target class
Nucleic acid metabolism
Target subclass
Phosphodiesterase
Control
cpd 3
Recommended Cell Concentration
None
Source data