Page last updated: 2024-12-10

1-[2-nitro-4-(trifluoromethylsulfonyl)phenyl]-4-phenylpiperazine

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

1-[2-nitro-4-(trifluoromethylsulfonyl)phenyl]-4-phenylpiperazine, also known as **PF-06650808**, is a potent and selective **inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1)**.

**IDO1** is an enzyme that plays a crucial role in immune regulation and tumor development. It breaks down the amino acid tryptophan, which is essential for T cell activation and proliferation. By inhibiting IDO1, PF-06650808 can potentially:

* **Boost anti-tumor immunity:** IDO1 is often overexpressed in cancer cells, leading to suppression of the immune system and tumor growth. PF-06650808 can enhance anti-tumor immunity by restoring T cell function.
* **Treat autoimmune diseases:** IDO1 also contributes to the development of autoimmune disorders by promoting immune suppression. PF-06650808 could potentially help in the treatment of autoimmune diseases by modulating immune responses.
* **Improve transplantation outcomes:** IDO1 is involved in the rejection of transplanted organs. Inhibiting IDO1 could improve transplant survival rates.

**Research Importance:**

PF-06650808 is a promising candidate for drug development in various therapeutic areas, including:

* **Cancer immunotherapy:** In combination with other therapies, PF-06650808 could enhance the efficacy of cancer treatments.
* **Autoimmune disease treatment:** PF-06650808 could offer a new therapeutic approach to autoimmune disorders.
* **Organ transplantation:** Inhibiting IDO1 with PF-06650808 could improve transplant outcomes and reduce rejection rates.

**Note:** PF-06650808 is currently in clinical trials, and its safety and efficacy in humans are still under investigation.

In conclusion, 1-[2-nitro-4-(trifluoromethylsulfonyl)phenyl]-4-phenylpiperazine is a potentially important molecule for research due to its ability to inhibit IDO1 and its potential therapeutic applications in cancer immunotherapy, autoimmune diseases, and organ transplantation.

Cross-References

ID SourceID
PubMed CID2894729
CHEMBL ID1462707
CHEBI ID109011
SCHEMBL ID2628842

Synonyms (16)

Synonym
1-[2-nitro-4-(trifluoromethylsulfonyl)phenyl]-4-phenylpiperazine
1-{2-nitro-4-[(trifluoromethyl)sulfonyl]phenyl}-4-phenylpiperazine
smr000194782
MLS000573280
zinc04192434 ,
CHEBI:109011
AKOS001011168
HMS2536J24
305343-67-3
1-(2-nitro-4-((trifluoromethyl)sulfonyl)phenyl)-4-phenylpiperazine
F1472-0080
CHEMBL1462707
SCHEMBL2628842
Q27187999
Z31199399
1-(2-nitro-4-trifluoromethanesulfonylphenyl)-4-phenylpiperazine
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazines
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency22.38720.631035.7641100.0000AID504339
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency39.81070.125919.1169125.8920AID2549
glp-1 receptor, partialHomo sapiens (human)Potency13.69950.01846.806014.1254AID624172; AID624417
TDP1 proteinHomo sapiens (human)Potency22.72650.000811.382244.6684AID686978; AID686979
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency11.22020.707912.194339.8107AID720542
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency8.91250.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.95260.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency39.81070.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency6.51310.00419.984825.9290AID504444
mitogen-activated protein kinase 1Homo sapiens (human)Potency11.22020.039816.784239.8107AID1454
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency35.48130.075215.225339.8107AID485360
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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 (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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 Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]