Page last updated: 2024-12-11
nigakinone
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
nigakinone: an NSAID that may be useful in treating ulcerative colitis; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5320161 |
| CHEMBL ID | 1594741 |
| CHEBI ID | 81365 |
| SCHEMBL ID | 5664418 |
| MeSH ID | M0534147 |
Synonyms (26)
| Synonym |
|---|
| MLS000574953 |
| smr001215932 |
| 4-methoxy-5-hydroxycanthin-6-one |
| nigakinone |
| C17879 |
| 18110-86-6 |
| HMS2269C08 |
| unii-j7e73434d2 |
| J7E73434D2 , |
| 5-hydroxy-4-methoxycanthin-6-one |
| 6h-indolo(3,2,1-de)(1,5)naphthyridin-6-one, 5-hydroxy-4-methoxy- |
| CHEBI:81365 , |
| SCHEMBL5664418 |
| CHEMBL1594741 |
| AC-34395 |
| 5-hydroxy-4-methoxy-6h-indolo[3,2,1-de][1,5]naphthyridin-6-one |
| PGFKZUOYIFDMQJ-UHFFFAOYSA-N |
| HY-N2128 |
| CS-0018679 |
| 4-methoxy-1,6-diazatetracyclo[7.6.1.0^{5,16.0^{10,15]hexadeca-4,7,9(16),10,12,14-hexaene-2,3-dione |
| Q27155302 |
| FT-0701509 |
| 3-hydroxy-4-methoxy-1,6-diazatetracyclo[7.6.1.05,16.010,15]hexadeca-3,5(16),6,8,10,12,14-heptaen-2-one |
| MS-23755 |
| 6h-indolo[3,2,1-de][1,5]naphthyridin-6-one, 5-hydroxy-4-methoxy- |
| E80697 |
Research Excerpts
Effects
| Excerpt | Reference | Relevance |
|---|---|---|
| "Nigakinone has potential therapeutic effects on colitis." | ( Nigakinone alleviates DSS-induced experimental colitis via regulating bile acid profile and FXR/NLRP3 signaling pathways. Lin, C; Liu, F; Wang, M; Wang, Q; Yao, Y; Zhang, F; Zhu, C, 2023) | 3.07 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dysfunction of copper homeostasis can lead to a host of disorders, which might be toxic sometimes." | ( In vivo toxic effects of 4-methoxy-5-hydroxy-canthin-6-one in zebrafish embryos via copper dyshomeostasis and oxidative stress. Feng, F; Gong, G; He, MF; Jiang, L; Lin, Q; Liu, W; Qu, W; Xie, N; Zhang, J, 2018) | 0.48 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| "The pharmacokinetic results showed that the prototype of PQ-A was the main existing form in both physiological and pathological conditions." | ( A comparative study on pharmacokinetics and tissue distribution of 5-hydroxy-4-methoxycanthin-6-one and its metabolite in normal and dextran sodium sulfate-induced colitis rats by HPLC-MS/MS. Lin, C; Liu, C; Liu, F; Wang, M; Yao, Y; Zhang, Q; Zhu, C, 2020) | 0.56 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| beta-carbolines | Any pyridoindole containing a beta-carboline skeleton and their hydrogenated derivatives |
| [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 (13)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 79.4328 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 39.8107 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
| GLS protein | Homo sapiens (human) | Potency | 35.4813 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 3.9811 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
| Smad3 | Homo sapiens (human) | Potency | 31.6228 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.5481 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 27.0050 | 5.8048 | 36.1306 | 65.1308 | AID540253; AID540263 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 11.2202 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| snurportin-1 | Homo sapiens (human) | Potency | 27.0050 | 5.8048 | 36.1306 | 65.1308 | AID540253; AID540263 |
| GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 5.8048 | 16.9962 | 25.9290 | AID540253 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 22.2775 | 0.0501 | 27.0736 | 89.1251 | AID588590; AID720496 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 35.4813 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 1.1220 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (23)
Molecular Functions (12)
Ceullar Components (10)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| intracellular non-membrane-bounded organelle | TAR DNA-binding protein 43 | Homo sapiens (human) |
| nucleus | TAR DNA-binding protein 43 | Homo sapiens (human) |
| nucleoplasm | TAR DNA-binding protein 43 | Homo sapiens (human) |
| perichromatin fibrils | TAR DNA-binding protein 43 | Homo sapiens (human) |
| mitochondrion | TAR DNA-binding protein 43 | Homo sapiens (human) |
| cytoplasmic stress granule | TAR DNA-binding protein 43 | Homo sapiens (human) |
| nuclear speck | TAR DNA-binding protein 43 | Homo sapiens (human) |
| interchromatin granule | TAR DNA-binding protein 43 | Homo sapiens (human) |
| nucleoplasm | TAR DNA-binding protein 43 | Homo sapiens (human) |
| chromatin | TAR DNA-binding protein 43 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (19)
| 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. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1320174 | Cerebral protective activity in anesthetized cerebral ischemia-induced Mongolian gerbil hippocampus assessed as protective values on density of surviving neurons in CA1 subfields of hippocampus at 100 mg/kg, po pretreated for 30 mins followed by bilateral | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Evaluation of canthinone alkaloids as cerebral protective agents. |
| AID1194597 | Inhibition of PTP1B (unknown origin) assessed as inhibition rate at 100 uM | 2015 | Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9 | Canthinone alkaloids are novel protein tyrosine phosphatase 1B inhibitors. |
| AID1320173 | Cerebral protective activity in cerebral ischemia-induced Mongolian gerbil assessed as passive avoidance test value at 100 mg/kg, po pretreated for 30 mins followed by bilateral ligation-induced ischemia for 5 mins measured on day 1 post 3 days ischemia i | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Evaluation of canthinone alkaloids as cerebral protective agents. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (14)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (14.29) | 29.6817 |
| 2010's | 7 (50.00) | 24.3611 |
| 2020's | 5 (35.71) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.94
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 (11.94) All Compounds (24.57) |
Study Types
| 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 | 14 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||