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.
ID Source | ID |
---|---|
PubMed CID | 2894729 |
CHEMBL ID | 1462707 |
CHEBI ID | 109011 |
SCHEMBL ID | 2628842 |
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 |
Class | Description |
---|---|
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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 22.3872 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 39.8107 | 0.1259 | 19.1169 | 125.8920 | AID2549 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 13.6995 | 0.0184 | 6.8060 | 14.1254 | AID624172; AID624417 |
TDP1 protein | Homo sapiens (human) | Potency | 22.7265 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 11.2202 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 8.9125 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 19.9526 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 6.5131 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 11.2202 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 35.4813 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 35.4813 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 (12.56) All Compounds (24.57) |
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 | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |