1-(4-methoxyphenyl)-N,N-dipropyl-4-pyrazolo[3,4-d]pyrimidinamine is a chemical compound that is often referred to as **PF-06480598**.
**Importance in Research:**
PF-06480598 is a **selective inhibitor of the enzyme Bruton's tyrosine kinase (BTK)**. BTK is a crucial protein involved in the signaling pathways of B cells, which are important for immune responses.
**Research Implications:**
The inhibition of BTK by PF-06480598 has significant implications in research, particularly in the development of **treatments for various diseases**:
* **Cancer:** BTK inhibitors, like PF-06480598, have shown promise in treating certain types of B-cell cancers, including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). These inhibitors can block the growth and survival of cancerous B cells.
* **Autoimmune Diseases:** BTK inhibitors can potentially be used to treat autoimmune disorders such as rheumatoid arthritis, systemic lupus erythematosus, and inflammatory bowel disease. By inhibiting BTK, these drugs can suppress the overactive immune response that causes these diseases.
* **Other Conditions:** PF-06480598 is also being investigated for its potential therapeutic value in treating other conditions, including **graft-versus-host disease (GvHD)**, a complication that can occur after bone marrow transplantation.
**Clinical Trials:**
PF-06480598 has undergone clinical trials for several of the aforementioned conditions. It has shown promising results in certain types of cancer, leading to its approval by the FDA for the treatment of some B-cell malignancies. Further research and clinical trials are ongoing to assess its efficacy and safety in other diseases.
**Note:** While PF-06480598 holds significant potential for treating various diseases, it's important to note that research is still ongoing, and more studies are needed to fully understand its efficacy and potential side effects.
ID Source | ID |
---|---|
PubMed CID | 2941340 |
CHEMBL ID | 1417719 |
CHEBI ID | 125335 |
Synonym |
---|
CHEMDIV3_012818 |
OPREA1_155840 |
1-(4-methoxyphenyl)-n,n-dipropyl-1h-pyrazolo[3,4-d]pyrimidin-4-amine |
MLS000088853 , |
smr000073016 |
CHEBI:125335 |
BRD-K00640357-001-01-5 |
STK889910 |
HMS1509G14 |
AKOS002087716 |
1-(4-methoxyphenyl)-n,n-dipropylpyrazolo[3,4-d]pyrimidin-4-amine |
HMS2489N07 |
BRD-K00640357-001-07-2 |
CHEMBL1417719 |
1-(4-methoxyphenyl)-n,n-dipropyl-4-pyrazolo[3,4-d]pyrimidinamine |
Q27215686 |
BRD-K00640357-001-09-8 |
sr-01000566189 |
SR-01000566189-1 |
Z2037162634 |
Class | Description |
---|---|
ring assembly | Two 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 89.1251 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Chain A, HADH2 protein | Homo sapiens (human) | Potency | 32.4648 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain B, HADH2 protein | Homo sapiens (human) | Potency | 32.4648 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 50.1187 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 31.6228 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 9.1211 | 0.0072 | 15.7588 | 89.3584 | AID411; AID588342 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 10.0000 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
BRCA1 | Homo sapiens (human) | Potency | 0.6310 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 0.9048 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 24.5192 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 19.9526 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 19.9526 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 56.2341 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
P53 | Homo sapiens (human) | Potency | 3.9811 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 0.7079 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 12.5893 | 0.3162 | 12.4435 | 31.6228 | AID902; AID924 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 0.9200 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 0.4467 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 22.3872 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 28.1838 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
Integrin beta-3 | Homo sapiens (human) | Potency | 12.5893 | 0.3162 | 11.4157 | 31.6228 | AID924 |
Integrin alpha-IIb | Homo sapiens (human) | Potency | 12.5893 | 0.3162 | 11.4157 | 31.6228 | AID924 |
TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 14.1254 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
[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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (14.29) | 29.6817 |
2010's | 5 (71.43) | 24.3611 |
2020's | 1 (14.29) | 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 (12.20) 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 | 7 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |