Page last updated: 2024-12-09

1-[1-(4-methoxyphenyl)-4-pyrazolo[3,4-d]pyrimidinyl]-4-piperidinecarboxamide

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

**1-[1-(4-methoxyphenyl)-4-pyrazolo[3,4-d]pyrimidinyl]-4-piperidinecarboxamide** is a chemical compound, also known by its shorter name, **PF-06651600**. It is a potent and selective inhibitor of **JAK3**, an enzyme involved in the immune system.

**Importance for Research:**

**1. Targeting JAK3 for Immunomodulation:**

* JAK3 plays a critical role in the signaling pathways of various immune cells, including T cells and natural killer cells.
* Inhibition of JAK3 can disrupt these signaling pathways, leading to immunosuppression.

**2. Potential Therapeutic Applications:**

* **Autoimmune Diseases:** PF-06651600 has shown promising results in preclinical studies for treating autoimmune diseases such as rheumatoid arthritis, lupus, and inflammatory bowel disease.
* **Organ Transplantation:** JAK3 inhibition can suppress immune rejection in organ transplantation.
* **Cancer:** Some studies suggest that JAK3 inhibition may have potential in treating certain cancers.

**3. Understanding JAK3 Signaling:**

* PF-06651600 is a valuable tool for researchers studying the role of JAK3 in various biological processes.
* It helps elucidate the mechanisms of JAK3 signaling and its impact on immune responses.

**4. Drug Development:**

* PF-06651600 is currently in clinical trials for various therapeutic applications.
* It is a promising candidate for developing new drugs that target JAK3 for the treatment of immune-related diseases.

**Overall, PF-06651600 is an important research tool and potential therapeutic agent due to its selective inhibition of JAK3, which offers promising therapeutic avenues for treating autoimmune diseases, preventing organ rejection, and potentially combating certain cancers.**

**Note:** The information provided here is for educational purposes only and should not be considered medical advice. It is essential to consult with a healthcare professional for any medical concerns.

Cross-References

ID SourceID
PubMed CID661360
CHEMBL ID1527862
CHEBI ID123271

Synonyms (17)

Synonym
MLS001306219
OPREA1_128935
smr000035752
MLS000036774 ,
NCGC00019895-01
CHEBI:123271
1-[1-(4-methoxyphenyl)pyrazolo[3,4-d]pyrimidin-4-yl]piperidine-4-carboxamide
NCGC00019895-02
HMS2402M12
AKOS022118014
STL336656
1-[1-(4-methoxyphenyl)-1h-pyrazolo[3,4-d]pyrimidin-4-yl]piperidine-4-carboxamide
CHEMBL1527862
1-[1-(4-methoxyphenyl)-4-pyrazolo[3,4-d]pyrimidinyl]-4-piperidinecarboxamide
Q27212975
SR-01000003250-2
sr-01000003250
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
pyrazoles
[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 (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency15.10140.007215.758889.3584AID588342
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
TDP1 proteinHomo sapiens (human)Potency0.58050.000811.382244.6684AID686979
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency3.54810.01262.451825.0177AID485313
vasopressin V1b receptorHomo sapiens (human)Potency24.52970.194416.018043.6206AID492948
DNA polymerase betaHomo sapiens (human)Potency35.48130.022421.010289.1251AID485314
ras-related protein Rab-9AHomo sapiens (human)Potency2.81840.00022.621531.4954AID485297
relaxin receptor 1 isoform 1Homo sapiens (human)Potency32.08740.038814.350143.6206AID2676; AID489012; AID492949
relaxin receptor 2 isoform 1Homo sapiens (human)Potency19.48460.048815.980148.9431AID489043
Guanine nucleotide-binding protein GHomo sapiens (human)Potency50.11871.995325.532750.1187AID624287
[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
AID651635Viability Counterscreen for Primary 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.
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.
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.
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.
[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]