Page last updated: 2024-12-09

1-(4-methoxyphenyl)-N-[2-(4-morpholinyl)ethyl]-4-pyrazolo[3,4-d]pyrimidinamine

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

1-(4-methoxyphenyl)-N-[2-(4-morpholinyl)ethyl]-4-pyrazolo[3,4-d]pyrimidinamine is a chemical compound often referred to as **Pazopanib**.

**Pazopanib** is a **tyrosine kinase inhibitor**, which means it blocks the activity of certain enzymes called tyrosine kinases. These enzymes play a crucial role in cell signaling and growth. Pazopanib specifically targets several tyrosine kinases, including:

* **VEGFRs (Vascular Endothelial Growth Factor Receptors):** These receptors are involved in the formation of new blood vessels (angiogenesis), a process crucial for tumor growth.
* **PDGFRs (Platelet-Derived Growth Factor Receptors):** These receptors are involved in cell proliferation and survival, which can contribute to tumor growth.
* **c-KIT:** This receptor is involved in cell development and proliferation, and it is often overexpressed in certain cancers.

**Why Pazopanib is Important for Research:**

Pazopanib is important for research due to its potential therapeutic applications in various areas:

* **Cancer Treatment:** Pazopanib has been approved by the FDA for treating **renal cell carcinoma (RCC)** and **soft tissue sarcomas**. It works by inhibiting the growth of cancer cells by blocking the signaling pathways that promote their proliferation and survival.
* **Other Potential Applications:** Pazopanib is being studied in clinical trials for other types of cancer, including **breast cancer, colorectal cancer, and lung cancer**. It is also being investigated for its potential use in treating **rheumatoid arthritis, inflammatory bowel disease, and diabetic retinopathy**.
* **Understanding of Tyrosine Kinase Inhibition:** The study of Pazopanib and other tyrosine kinase inhibitors has contributed significantly to our understanding of how these enzymes function and how their inhibition can be therapeutically beneficial. This knowledge is crucial for the development of new and more effective therapies for a range of diseases.

**Overall, Pazopanib is a significant molecule in the field of cancer research and therapy. Its effectiveness in treating certain cancers and its potential for other therapeutic applications make it an important subject of ongoing research.**

Cross-References

ID SourceID
PubMed CID1985423
CHEMBL ID1472430
CHEBI ID107981

Synonyms (15)

Synonym
MLS000556538
[1-(4-methoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-4-yl]-(2-morpholin-4-yl-ethyl)-amine
smr000147855
OPREA1_318047
CHEBI:107981
1-(4-methoxyphenyl)-n-(2-morpholin-4-ylethyl)pyrazolo[3,4-d]pyrimidin-4-amine
HMS2357F12
AKOS022118018
CHEMBL1472430
1-(4-methoxyphenyl)-n-[2-(morpholin-4-yl)ethyl]-1h-pyrazolo[3,4-d]pyrimidin-4-amine
STL336444
1-(4-methoxyphenyl)-n-[2-(4-morpholinyl)ethyl]-4-pyrazolo[3,4-d]pyrimidinamine
Q27186336
SR-01000566503-1
sr-01000566503
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency28.18380.044717.8581100.0000AID485294
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency15.10140.007215.758889.3584AID588342
ATAD5 protein, partialHomo sapiens (human)Potency12.45180.004110.890331.5287AID504466; AID504467
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency14.12540.011212.4002100.0000AID1030
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency79.43280.035520.977089.1251AID504332
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency20.59620.00419.984825.9290AID504444
ras-related protein Rab-9AHomo sapiens (human)Potency5.62340.00022.621531.4954AID485297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1745845Primary 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]