1-(3-methylphenyl)-N-(2-pyridinylmethyl)-4-pyrazolo[3,4-d]pyrimidinamine, also known as **GSK2881073**, is a potent and selective inhibitor of **Janus kinase 3 (JAK3)**.
**Why it's important for research:**
* **JAK3 Inhibition and Immune Regulation:** JAK3 is a crucial enzyme involved in the signaling pathways of various immune cells, particularly T cells and natural killer cells. Its inhibition has been shown to suppress immune responses, making GSK2881073 a potential therapeutic target for autoimmune diseases and organ transplant rejection.
* **Autoimmune Disease Treatment:** GSK2881073 has been studied extensively in clinical trials for the treatment of **rheumatoid arthritis**, **psoriasis**, and **Crohn's disease**. Its selectivity for JAK3 over other JAK kinases makes it a promising candidate for minimizing adverse effects often associated with broader JAK inhibition.
* **Organ Transplantation:** Inhibiting JAK3 can also help prevent graft rejection in organ transplantation. GSK2881073 is being investigated for its potential to improve graft survival and reduce the need for immunosuppressive drugs.
* **Cancer Research:** JAK3 is implicated in the development and progression of some cancers. While its role in cancer is not fully understood, GSK2881073 and other JAK3 inhibitors are being explored as potential anticancer agents.
**Further Research and Development:**
While GSK2881073 has shown promising results in early clinical trials, its development is ongoing. Researchers are investigating its long-term efficacy, safety, and optimal dosage for different conditions.
**Note:** It's important to understand that GSK2881073 is still in clinical development and is not currently approved for any therapeutic use.
ID Source | ID |
---|---|
PubMed CID | 697693 |
CHEMBL ID | 1568193 |
CHEBI ID | 122064 |
Synonym |
---|
OPREA1_669568 |
AKOS002381533 |
smr000017435 |
MLS000098831 |
OPREA1_436203 |
MLS000100851 , |
CHEBI:122064 |
1-(3-methylphenyl)-n-(pyridin-2-ylmethyl)pyrazolo[3,4-d]pyrimidin-4-amine |
1-(3-methylphenyl)-n-(pyridin-2-ylmethyl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine |
STK889860 |
AB00420405-05 |
HMS2279F06 |
393820-44-5 |
F0521-0048 |
n-(pyridin-2-ylmethyl)-1-(m-tolyl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine |
CHEMBL1568193 |
Q27210695 |
1-(3-methylphenyl)-n-(2-pyridinylmethyl)-4-pyrazolo[3,4-d]pyrimidinamine |
Z56992534 |
SR-01000566427-1 |
sr-01000566427 |
1-(3-methylphenyl)-n-[(pyridin-2-yl)methyl]-1h-pyrazolo[3,4-d]pyrimidin-4-amine |
Class | Description |
---|---|
pyrazoles | |
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. |
[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, HADH2 protein | Homo sapiens (human) | Potency | 19.9526 | 0.0251 | 20.2376 | 39.8107 | AID893 |
Chain B, HADH2 protein | Homo sapiens (human) | Potency | 19.9526 | 0.0251 | 20.2376 | 39.8107 | AID893 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 19.9526 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 26.8545 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
BRCA1 | Homo sapiens (human) | Potency | 11.2202 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
ClpP | Bacillus subtilis | Potency | 19.9526 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 20.5962 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 18.4782 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 1.5849 | 0.1800 | 13.5574 | 39.8107 | AID1468 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 14.1254 | 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 |
P53 | Homo sapiens (human) | Potency | 50.1187 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 0.0018 | 15.6638 | 39.8107 | AID894 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 3.5481 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
[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 | 4 (57.14) | 24.3611 |
2020's | 2 (28.57) | 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 (12.22) 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] |