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 Source | ID |
|---|---|
| PubMed CID | 14399 |
| CHEMBL ID | 1406831 |
| SCHEMBL ID | 6661149 |
| MeSH ID | M0145598 |
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
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 44.6684 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| TDP1 protein | Homo sapiens (human) | Potency | 10.5974 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 50.1187 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 29.9349 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 100.0000 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
| geminin | Homo sapiens (human) | Potency | 29.0929 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 17.7828 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 7.0795 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (5)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| cellular response to glucagon stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Molecular Functions (2)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (1)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (13)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID651635 | Viability 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (28.57) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (14.29) | 29.6817 |
| 2010's | 3 (42.86) | 24.3611 |
| 2020's | 1 (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.
| This Compound (12.06) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||