General
Preferred name
PF-06447475
Synonyms
PF 06447475 ()
PF06447475 ()
P&D ID
PD012846
CAS
1527473-33-1
Tags
available
drug candidate
Drug indication
Discovery agent
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
PF-06447475 was reported as a potent, brain-pentrant inhibitor of the serine-threonine kinase, leucine-rich repeat kinase 2 (LRRK2) . The compound's pharmacokinetic properties halted its progress towards clinical development, but it is a useful tool for the investigation of central and peripheral LRRK2 function in experimental models of Parkinson's disease for example .
(GtoPdb)
DESCRIPTION
PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.
PRICE
46
DESCRIPTION
Potent LRRK2 inhibitor; neuroprotective
(Tocriscreen Plus)
DESCRIPTION
PF06447475 is a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. Leucine rich repeat kinase 2 (LRRK2) has been genetically linked to Parkinson's disease (PD) by genome-wide association studies (GWAS). The most common LRRK2 mutation, G2019S, which is relatively rare in the total population, gives rise to increased kinase activity. As such, LRRK2 kinase inhibitors are potentially useful in the treatment of PD.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
14
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
15
Molecular Weight
305.13
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
2
Ring Count
4
Aromatic Ring Count
3
cLogP
2.33
TPSA
77.83
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
6.0
QED
0.79
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
G2019S LRRK2
LRRK2
LRRK2 inhibitor
MOA
serine/threonine kinase inhibitor
Pathway
Autophagy
Recommended Cell Concentration
100 nM
Source data
