General
Preferred name
PF-04457845
Synonyms
PF04457845 ()
PF 04457845 ()
cpd 23 ()
PF-4457845 ()
Redafamdastat ()
P&D ID
PD012760
CAS
1020315-31-4
Tags
available
free of charge
probe
covalent binder
drug candidate
Drug indication
Liver disease
Post-traumatic stress disorder
Drug Status
investigational
Max Phase
2.0
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
protein-selective
Probe sources
Chemical Probes.org
High-quality chemical probes
Open Science Probes
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)
COMMENT An excellent and very selective irreversible inhibitor of FAAH. Preincubation in vitro for 60 min is required to obtain maximum potency. Excellent brain penetration and efficacy with long duration of action after p.o, or i.p. dosing. Target engagement determined with fluorescent probe analogs. May 6 2021 - 10:43am
DESCRIPTION PF-04457845 is a highly selective, irreversible, covalent inactivator of fatty acid amide hydrolase (FAAH) , that is being investigated in clinical trials. It is one example from a dense analogoue series from patents (see 'Similar Compounds' in PubChem). (GtoPdb)
DESCRIPTION Redafamdastat (PF-04457845) is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2¡À0.63 nM and 7.4¡À0.62 nM for hFAAH and rFAAH, respectively.
PRICE 75
DESCRIPTION PF-04457845 is a greatly and effctive FAAH inhibitor, and for hFAAH(IC50=7.2??0.63 nM) and rFAAH(IC50=7.4??0.62 nM).
MOA Covalent Inhibitor (Chemical Probes.org)
DESCRIPTION Pan-histone demethylase inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION PF-04457845 is an excellent and very selective irreversible inhibitor of FAAH. It shows an excellent brain penetration and efficacy with long duration of action after p.o, or i.p. dosing. (Enamine Bioactive Compounds)
DESCRIPTION PF-04457845 is a greatly and effctive FAAH inhibitor, and for hFAAH(IC50=7.2±0.63 nM) and rFAAH(IC50=7.4±0.62 nM). (TargetMol Bioactive Compound Library)
Compound Sets
20
AdooQ Bioactive Compound Library
A15209
Cayman Chemical Bioactives
19306
ChEMBL Drugs
CHEMBL1651534
Chemical Probes.org
pf-04457845
CovalentInDB
CI000727
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12012
DrugMAP
DMPRYU1
Enamine Bioactive Compounds
EBC-420074
EU-OPENSCREEN Bioactive Compound Library
EOS101550
EUbOPEN Chemogenomics Library
EUB0000306
Guide to Pharmacology
6694
High-quality chemical probes
PD012760
MedChem Express Bioactive Compound Library
HY-14376
Open Science Probes
PF-04457845
ReFrame library
Selleckchem Bioactive Compound Library
pf-04457845
TargetMol Bioactive Compound Library
T4323
Tocris Bioactive Compound Library
6374
External IDs
26
Properties
(calculated by RDKit )
Molecular Weight
455.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
5.39
TPSA
80.24
Fraction CSP3
0.22
Chiral centers
0.0
Largest ring
6.0
QED
0.57
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Primary Target
Fatty Acid Amide Hydrolase
MOA
Inhibitor
FAAH inhibitor
Targeted domain
Active site (Ser241)
Target
FAAH
hFAAH
rFAAH
Pathway
Autophagy
Metabolism
Neuroscience
Metabolic Enzyme/Protease
Neuronal Signaling
Orthogonal probe
PF-3845
Control name
PF-04875474
Target class
Lipid metabolism
Target subclass
Serine Hydrolase
Recommended Cell Concentration
1 uM
Source data