Page last updated: 2024-11-12

azd3241

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

AZD3241: a myeloperoxidase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11528958
CHEMBL ID4297594
SCHEMBL ID1536607
SCHEMBL ID23225670
MeSH IDM000611635

Synonyms (44)

Synonym
1-(2-isopropoxyethyl)-2-thioxo-1,2,3,5-tetrahydro-pyrrolo[3,2-d]pyrimidin-4-one
FVJCUZCRPIMVLB-UHFFFAOYSA-N
SCHEMBL1536607
TT3345YXVR ,
azd3241
verdiperstat [inn]
bhv-3241
1-(2-isopropoxyethyl)-2-thioxo-1,2,3,5-tetrahydro-pyrrolo(3,2-d) pyrimidin-4-one
1-(2-isopropoxyethyl)-2-thioxo-1,2,3,5-tetrahydropyrrolo(3,2-d)pyrimidin-4-one
verdiperstat [who-dd]
verdiperstat
890655-80-8
azd 3241 [who-dd]
verdiperstat [usan]
azd-3241
CS-0016916
HY-17646
unii-tt3345yxvr
bhv-3421
who 10251
bdbm50503707
1-(2-propan-2-yloxyethyl)-2-sulfanylidene-5h-pyrrolo[2,3-e]pyrimidin-4-one
gtpl10052
azd 3241
DB12440
1-[2-(propan-2-yloxy)ethyl]-2-sulfanylidene-1,2,3,5-tetrahydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
1-(2-isopropoxyethyl)-2-thioxo-2,3-dihydro-1h-pyrrolo[3,2-d]pyrimidin-4(5h)-one
BS-17783
azd-3241; azd 3241; azd3241
BCP30847
azd3241;bhv-3241
verdiperstat (azd3241)
D11684
verdiperstat (usan/inn)
w4y ,
1-{2-[(propan-2-yl)oxy]ethyl}-2-sulfanylidene-1,2,3,5-tetrahydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
N16816
Q27290286
CHEMBL4297594
AKOS037649278
SCHEMBL23225670
EX-A3205
1-(2-propan-2-yloxyethyl)-2-sulfanylidene-5h-pyrrolo[3,2-d]pyrimidin-4-one
1-[2-(propan-2-yloxy)ethyl]-2-sulfanylidene-1h,2h,3h,4h,5h-pyrrolo[3,2-d]pyrimidin-4-one

Research Excerpts

Overview

AZD3241 is a potent and selective myeloperoxidase inhibitor potentially for the treatment of a number of neurodegenerative disorders, including multiple system atrophy.

ExcerptReferenceRelevance
"AZD3241 is a potent and selective myeloperoxidase inhibitor potentially for the treatment of a number of neurodegenerative disorders, including multiple system atrophy (MSA). "( Population Pharmacokinetic Modeling With Enterohepatic Circulation for AZD3241 in Healthy Subjects and Patients With Multiple System Atrophy.
Al-Huniti, N; Li, J; Li, Y; Mullen, JA; Savage, A; Taylor, W; Tong, X; Xu, H; Zhou, D, 2018
)
2.16

Pharmacokinetics

ExcerptReferenceRelevance
" The objectives of this work were to develop a population pharmacokinetic (PopPK) model for AZD3241 and to investigate the correlation between AZD3241 exposure and myeloperoxidase inhibition."( Population Pharmacokinetic Modeling With Enterohepatic Circulation for AZD3241 in Healthy Subjects and Patients With Multiple System Atrophy.
Al-Huniti, N; Li, J; Li, Y; Mullen, JA; Savage, A; Taylor, W; Tong, X; Xu, H; Zhou, D, 2018
)
0.93

Bioavailability

ExcerptReferenceRelevance
" The enterohepatic circulation model reasonably captured the second peak of AZD3241, and high-fat food increased the absorption rate by 69%."( Population Pharmacokinetic Modeling With Enterohepatic Circulation for AZD3241 in Healthy Subjects and Patients With Multiple System Atrophy.
Al-Huniti, N; Li, J; Li, Y; Mullen, JA; Savage, A; Taylor, W; Tong, X; Xu, H; Zhou, D, 2018
)
0.94
" Derived from an indole-containing high-throughput screen hit, optimization efforts resulted in potent and selective 6-substituted indoles with good oral bioavailability and in vivo activity."( Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).
Axford, L; Cohick, E; Dales, N; Deng, L; Hamann, LG; Harrison, TJ; Hollis-Symynkywicz, M; Kecman, S; Lee, L; Loi, S; Marcinkeviciene, J; Marro, ML; Papillon, JPN; Patnaik, A; Patterson, AW; Regard, JB; Ren, X, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
MyeloperoxidaseHomo sapiens (human)IC50 (µMol)0.63000.02001.88117.6800AID1514846; AID1663374
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
response to yeastMyeloperoxidaseHomo sapiens (human)
hypochlorous acid biosynthetic processMyeloperoxidaseHomo sapiens (human)
respiratory burst involved in defense responseMyeloperoxidaseHomo sapiens (human)
defense responseMyeloperoxidaseHomo sapiens (human)
response to oxidative stressMyeloperoxidaseHomo sapiens (human)
response to mechanical stimulusMyeloperoxidaseHomo sapiens (human)
removal of superoxide radicalsMyeloperoxidaseHomo sapiens (human)
response to foodMyeloperoxidaseHomo sapiens (human)
response to lipopolysaccharideMyeloperoxidaseHomo sapiens (human)
low-density lipoprotein particle remodelingMyeloperoxidaseHomo sapiens (human)
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
negative regulation of apoptotic processMyeloperoxidaseHomo sapiens (human)
defense response to fungusMyeloperoxidaseHomo sapiens (human)
response to gold nanoparticleMyeloperoxidaseHomo sapiens (human)
defense response to bacteriumMyeloperoxidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
chromatin bindingMyeloperoxidaseHomo sapiens (human)
peroxidase activityMyeloperoxidaseHomo sapiens (human)
protein bindingMyeloperoxidaseHomo sapiens (human)
heparin bindingMyeloperoxidaseHomo sapiens (human)
heme bindingMyeloperoxidaseHomo sapiens (human)
metal ion bindingMyeloperoxidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
extracellular regionMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
nucleusMyeloperoxidaseHomo sapiens (human)
nucleoplasmMyeloperoxidaseHomo sapiens (human)
lysosomeMyeloperoxidaseHomo sapiens (human)
secretory granuleMyeloperoxidaseHomo sapiens (human)
azurophil granule lumenMyeloperoxidaseHomo sapiens (human)
azurophil granuleMyeloperoxidaseHomo sapiens (human)
intracellular membrane-bounded organelleMyeloperoxidaseHomo sapiens (human)
extracellular exosomeMyeloperoxidaseHomo sapiens (human)
phagocytic vesicle lumenMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1663374Inhibition of myeloperoxidase (unknown origin)2020Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).
AID1514846Inhibition of MPO (unknown origin)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
The development of myeloperoxidase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (83.33)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.73

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index21.73 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (16.67%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]