General
Preferred name
mardepodect
Synonyms
PF-2545920 ()
PF-02545920 ()
Mardepodect (hydrochloride) ()
PF-2545920 (hydrochloride) ()
Mardepodect (PF-2545920) ()
PF-2545920 ()
MP-10 ()
PF-02545920 hydrochloride ()
Mardepodect hydrochloride ()
[11C]MP 10 ()
P&D ID
PD004447
CAS
1037309-45-7
1292799-56-4
898562-94-2
2070014-78-5
Tags
available
drug candidate
Drug indication
Schizophrenia
Huntington disease
Drug Status
investigational
Max Phase
2.0
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 PF-2545920 is a selective, orally active inhibitor of phosphodiesterase (PDE) 10A . Identified using structure-based drug design, the compound is optimised for selectivity, brain penetration and drug-like properties. Proposed INN is mardepodect. PF-2545920 is the first PDE10A inhibitor identified as a clinical lead utilizing this mechanism for the treatment of schizophrenia.
DESCRIPTION Mardepodect (PF-2545920) is a selective, orally active inhibitor of phosphodiesterase (PDE) 10A . Identified using structure-based drug design, the compound is optimised for selectivity, brain penetration and drug-like properties. PF-2545920 is the first PDE10A inhibitor identified as a clinical lead utilizing this mechanism for the treatment of schizophrenia. (GtoPdb)
DESCRIPTION Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier[1][2].
PRICE 123
DESCRIPTION Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier[1][2].
PRICE 230
DESCRIPTION Mardepodect hydrochloride (Mardepodect HCl) is an orally active, selective and potent inhibitor of PDE10A that crosses the blood-brain barrier (IC50: 0.37 nM).Mardepodect hydrochloride up-regulates the expression of proteins encoding specific growth and transcription factors, cell signalling molecules and cell surface proteins. Mardepodect hydrochloride upregulates genes encoding specific growth factors, transcription factors, cell signalling molecules, and cell surface proteins, while downregulating a broad spectrum of cell cycle and apoptosis-related genes.
PRICE 245
DESCRIPTION [11C]MP 10 (PF-2545920), a specific and effective PDE10A inhibitor (IC50=0.37 nM), is with more than1000-fold specificity activity over the PDE.
DESCRIPTION Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM and over 1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier. (TargetMol Bioactive Compound Library)
DESCRIPTION PF-02545920 is a potent inhibitor of phosphodiesterase 10A . It is selective for PDE10A over other PDEs. (Enamine Bioactive Compounds)
Cell lines
0
Organisms
1
Compound Sets
21
AdooQ Bioactive Compound Library
A11191
Cayman Chemical Bioactives
18266
ChEMBL Drugs
CHEMBL562318
Concise Guide to Pharmacology 2019/20
9617
Concise Guide to Pharmacology 2021/22
9617
Concise Guide to Pharmacology 2023/24
9617
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08387
DrugMAP
DMJPE61
Enamine Bioactive Compounds
EBC-767080
EU-OPENSCREEN Bioactive Compound Library
EOS100040
EUbOPEN Chemogenomics Library
EUB0002629
Guide to Pharmacology
9617
Mcule NIBR MoA Box Subset
MCULE-8681344563
MedChem Express Bioactive Compound Library
HY-50098
HY-50098A
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
pf-2545920
TargetMol Bioactive Compound Library
T16499
External IDs
37
Properties
(calculated by RDKit )
Molecular Weight
392.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
5
cLogP
5.28
TPSA
52.83
Fraction CSP3
0.08
Chiral centers
0.0
Largest ring
6.0
QED
0.41
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
PDE10A
Phosphodiesterase (PDE)
PDE
Member status
member
MOA
Phosphodiesterase 10A Inhibitors
phosphodiesterase inhibitor
Pathway
Metabolism
Metabolic Enzyme/Protease
Recommended Cell Concentration
1 uM
Source data