Page last updated: 2024-12-05

n-acetylmelphalan

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

Description

N-acetylmelphalan is a prodrug of melphalan, an alkylating agent used in the treatment of multiple myeloma. It is synthesized by acetylation of melphalan, which enhances its oral bioavailability. N-acetylmelphalan is converted to melphalan in the body, which then exerts its cytotoxic effects by alkylating DNA, thereby inhibiting cell division. Research on N-acetylmelphalan has focused on its potential to improve the efficacy and reduce the side effects of melphalan treatment. It is studied for its improved pharmacokinetic properties, which may translate to higher therapeutic efficacy and lower toxicity compared to melphalan.'

N-acetylmelphalan: RN given refers to (DL)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID14399
CHEMBL ID1406831
SCHEMBL ID6661149
MeSH IDM0145598

Synonyms (34)

Synonym
MLS000123340
smr000124012
1160-90-3
phenylalanine, n-acetyl-4-(bis(2-chloroethyl)amino)-
alanine, n-acetyl-3-(p-(bis(2-chloroethyl)amino)phenyl)-
2-acetylamino-3-{4-[bis-(2-chloro-ethyl)-amino]-phenyl}-propionic acid
n-acetylmelphalan
5786-56-1
nsc-212512
nsc154852
dl-phenylalanine, n-acetyl-4-[bis(2-chloroethyl)amino]-
nsc212512
n-acetylsarcolysine
nsc-154852
acetylsarcolysine
l-phenylalanine, n-acetyl-4-[bis(2-chloroethyl)amino]-
2-acetamido-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoic acid
AKOS000588937
NCGC00245095-01
HMS2470G07
alanine, n-acetyl-3-(p-(bis(2-chloroethyl)amino)phenyl)-, dl-
n-acmel
dl-phenylalanine, n-acetyl-4-(bis(2-chloroethyl)amino)-
nsc 212512
2-acetylamino-3-{4-[bis(2-chloroethyl)amino]phenyl}propionic acid
NZEYWBNQKCRBFO-UHFFFAOYSA-N
AKOS024304113
SCHEMBL6661149
CHEMBL1406831
SR-01000319133-1
sr-01000319133
n-acetyl-4-[bis(2-chloroethyl)amino]-dl-phenylalanine
DTXSID90921896
4-[bis(2-chloroethyl)amino]-n-(1-hydroxyethylidene)phenylalanine
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency44.66840.044717.8581100.0000AID485294
thioredoxin reductaseRattus norvegicus (Norway rat)Potency31.62280.100020.879379.4328AID588453
TDP1 proteinHomo sapiens (human)Potency10.59740.000811.382244.6684AID686978; AID686979
thioredoxin glutathione reductaseSchistosoma mansoniPotency50.11870.100022.9075100.0000AID485364
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency29.93490.707912.194339.8107AID720542
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency100.00000.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency29.09290.004611.374133.4983AID624296
lamin isoform A-delta10Homo sapiens (human)Potency17.78280.891312.067628.1838AID1487
Guanine nucleotide-binding protein GHomo sapiens (human)Potency7.07951.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (28.57)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's3 (42.86)24.3611
2020's1 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.06

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.06 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.14 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]