Page last updated: 2024-12-09

1-[(4-methylphenyl)methyl]-4-(1-pyrrolidinyl)pyrazolo[3,4-d]pyrimidine

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

You're describing a compound with the chemical name **1-[(4-methylphenyl)methyl]-4-(1-pyrrolidinyl)pyrazolo[3,4-d]pyrimidine**. This compound, often referred to by its shorthand name **PF-06700841**, is a potent and selective **inhibitor of the enzyme p38α MAP kinase**.

Here's why it's important in research:

* **p38α MAP kinase** is a critical enzyme involved in the inflammatory response. It's activated by various stressors, including inflammatory cytokines, bacterial toxins, and UV radiation.
* **Inflammation** plays a role in a wide range of diseases, including arthritis, inflammatory bowel disease, asthma, and even cancer.
* **PF-06700841** shows promise as a potential treatment for inflammatory diseases by blocking the activity of p38α MAP kinase.

**Key research findings:**

* **Preclinical studies** have shown that PF-06700841 can effectively suppress inflammation in various animal models.
* **Clinical trials** are ongoing to evaluate the safety and efficacy of PF-06700841 in humans with inflammatory diseases.

**Research implications:**

* PF-06700841 could potentially offer a new and effective treatment option for patients with inflammatory diseases.
* Further research into PF-06700841 and other p38α MAP kinase inhibitors could lead to a better understanding of inflammatory pathways and the development of novel therapies.

**Note:** It's important to remember that PF-06700841 is still under investigation and has not yet been approved for use in humans.

Cross-References

ID SourceID
PubMed CID895441
CHEMBL ID1392671
CHEBI ID121114

Synonyms (19)

Synonym
HMS1697L08
smr000074055
MLS000099456 ,
1-(4-methylbenzyl)-4-(1-pyrrolidinyl)-1h-pyrazolo[3,4-d]pyrimidine
1-(4-methylbenzyl)-4-(pyrrolidin-1-yl)-1h-pyrazolo[3,4-d]pyrimidine
STK101594
CHEBI:121114
AKOS000561857
1-[(4-methylphenyl)methyl]-4-pyrrolidin-1-ylpyrazolo[3,4-d]pyrimidine
HMS2186C22
F1405-0626
CHEMBL1392671
1-[(4-methylphenyl)methyl]-4-(1-pyrrolidinyl)pyrazolo[3,4-d]pyrimidine
Q27209359
VU0047470-1
sr-01000267934
SR-01000267934-1
1-{1-[(4-methylphenyl)methyl]-1h-pyrazolo[3,4-d]pyrimidin-4-yl}pyrrolidine
612524-17-1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyrazolopyrimidine
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency100.00000.044717.8581100.0000AID485294
glp-1 receptor, partialHomo sapiens (human)Potency11.51890.01846.806014.1254AID624172; AID624417
ATAD5 protein, partialHomo sapiens (human)Potency25.92900.004110.890331.5287AID504467
GLS proteinHomo sapiens (human)Potency15.84890.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency24.84460.000811.382244.6684AID686978; AID686979
pyruvate kinase PKM isoform aHomo sapiens (human)Potency12.58930.04017.459031.6228AID1631; AID1634
mitogen-activated protein kinase 1Homo sapiens (human)Potency12.58930.039816.784239.8107AID995
gemininHomo sapiens (human)Potency16.36010.004611.374133.4983AID624296
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (15)

Assay IDTitleYearJournalArticle
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
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.
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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[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-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's5 (71.43)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: 12.20

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 Index12.20 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.20)

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]