General
Preferred name
DSM-265
Synonyms
PfSPZ ()
DSM265 ()
Dsm265 ()
DSM 265 ()
P&D ID
PD058088
CAS
1282041-94-4
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
Drug indication
Malaria
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
DSM265 is a selective inhibitor of malarial dihydroorotate dehydrogenase (DHODH) in vitro and is active against both blood and liver stages of P. falciparum in vivo . Favorable pharmacokinetic properties have facilitated progression to clinical trial
DESCRIPTION
DSM265 is an optimised candidate from the triazolopyrimidine structural class and represents a new class of antimalarial drug. DSM265 is active against both asexual blood and liver stages of P. falciparum .
Favorable pharmacokinetic properties, compatible with single-dose treatment, have facilitated progression to clinical trial .
Potential Target/Mechanism Of Action: DSM265 is a selective inhibitor of malarial dihydroorotate dehydrogenase (DHODH) in vitro.
Favorable pharmacokinetic properties, compatible with single-dose treatment, have facilitated progression to clinical trial .
Potential Target/Mechanism Of Action: DSM265 is a selective inhibitor of malarial dihydroorotate dehydrogenase (DHODH) in vitro.
DESCRIPTION
DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM[1][2].
PRICE
80
DESCRIPTION
DSM265 is an optimised candidate and clinical lead from the triazolopyrimidine structural class and represents a new class of antimalarial drug .
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)
DESCRIPTION
DSM265 is a selective DHODH (dihydroorotate dehydrogenase) inhibitor used for prevention and treatment of malaria. DSM265 is highly selective toward DHODH of the malaria parasite Plasmodium. It is efficacious against both blood and liver stages of P. falciparum and active against drug-resistant parasite isolates. Treatment for malaria was in phase II clinical trials.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
DSM265 (PfSPZ) is a dihydroorotic acid dehydrogenase inhibitor with antimalarial activity (IC50: 8.9 nM).DSM265 inhibits the growth of Pf3D7 parasites and can be used for the treatment and prophylaxis of malaria infections.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
2
Compound Sets
10
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
ReFrame library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
21
Molecular Weight
415.07
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
3
cLogP
5.95
TPSA
55.11
Fraction CSP3
0.21
Chiral centers
0.0
Largest ring
6.0
QED
0.54
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
DHODH
P. falciparum
Dihydroorotate Dehydrogenase
Parasite
MOA
dihydroorotate dehydrogenase inhibitor
Pathway
Metabolism
Microbiology/virology
Anti-infection
Metabolic Enzyme/Protease
Solubility
Soluble in DMSO
Source data
