Page last updated: 2024-11-12
indoxam
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
indoxam: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9911907 |
| CHEMBL ID | 332993 |
| SCHEMBL ID | 5892140 |
| MeSH ID | M0305684 |
Synonyms (6)
| Synonym |
|---|
| (1-aminooxalyl-3-biphenyl-2-ylmethyl-2-ethyl-indolizin-8-yloxy)-acetic acid |
| bdbm50053137 |
| indoxam |
| 2-[2-ethyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid |
| CHEMBL332993 , |
| SCHEMBL5892140 |
Research Excerpts
Overview
Me-Indoxam is a previously discovered indole analogue that binds tightly to many sPLA(2)s. X-ray structure of the hGX-Me- Indoxam complex was determined at a resolution of 2.0 A.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Me-Indoxam is a previously discovered indole analogue that binds tightly to many sPLA(2)s, and the X-ray structure of the hGX-Me-Indoxam complex was determined at a resolution of 2.0 A." | ( Inhibition of the complete set of mammalian secreted phospholipases A(2) by indole analogues: a structure-guided study. Bahnson, BJ; Bollinger, JG; Gelb, MH; Pan, YH; Smart, BP; Weeks, AK, 2004) | 0.84 |
Actions
| Excerpt | Reference | Relevance |
|---|---|---|
| "Indoxam was found to suppress the elevation of the plasma level of TNF-alpha and prolonged the survival of endotoxin-challenged mice." | ( [Functional analysis of phospholipase A2 receptor by gene knockout studies]. Yokota, Y, 2001) | 1.03 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (14)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Group 10 secretory phospholipase A2 | Homo sapiens (human) | IC50 (µMol) | 1.6000 | 0.0410 | 0.1038 | 0.2000 | AID341251 |
| Phospholipase A2 | Homo sapiens (human) | IC50 (µMol) | 0.2363 | 0.0030 | 0.9122 | 3.9000 | AID158925; AID158926; AID341239 |
| Phospholipase A2, membrane associated | Homo sapiens (human) | IC50 (µMol) | 0.0230 | 0.0030 | 1.0811 | 8.0000 | AID1894717; AID1894718; AID341241 |
| Phospholipase A2, membrane associated | Mus musculus (house mouse) | IC50 (µMol) | 0.1500 | 0.0300 | 0.0800 | 0.1500 | AID341242 |
| Phospholipase A2 group V | Homo sapiens (human) | IC50 (µMol) | 0.1000 | 0.1000 | 0.2256 | 0.5000 | AID341249 |
| Phospholipase A2 group V | Mus musculus (house mouse) | IC50 (µMol) | 0.1700 | 0.1700 | 0.5475 | 0.7500 | AID341250 |
| Group IIF secretory phospholipase A2 | Homo sapiens (human) | IC50 (µMol) | 1.6000 | 0.1140 | 0.1250 | 0.1310 | AID341247 |
| Group IIE secretory phospholipase A2 | Homo sapiens (human) | IC50 (µMol) | 0.0100 | 0.0100 | 0.0710 | 0.1310 | AID341245 |
| Group IIE secretory phospholipase A2 | Mus musculus (house mouse) | IC50 (µMol) | 0.0350 | 0.0350 | 0.0617 | 0.0750 | AID341246 |
| Group 10 secretory phospholipase A2 | Mus musculus (house mouse) | IC50 (µMol) | 0.9000 | 0.0750 | 0.3500 | 0.9000 | AID341252 |
| Group IID secretory phospholipase A2 | Homo sapiens (human) | IC50 (µMol) | 1.3000 | 0.0600 | 0.1017 | 0.1310 | AID341243 |
| Group IID secretory phospholipase A2 | Mus musculus (house mouse) | IC50 (µMol) | 1.6000 | 0.4300 | 0.4300 | 0.4300 | AID341244 |
| Phospholipase A2 | Mus musculus (house mouse) | IC50 (µMol) | 1.0000 | 0.1400 | 0.4267 | 1.0000 | AID341240 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (81)
Molecular Functions (12)
Ceullar Components (18)
Bioassays (20)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID341243 | Inhibition of human group2D phospholipase A2 by [3H]oleic acid-labeled Escherichia coli membrane assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341238 | Inhibition of human group12A phospholipase A2 at 1.6 uM | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID1894717 | Inhibition of human group IIA phospholipase A2 incubated for 30 mins by automatic plate reader analysis | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities. |
| AID341242 | Inhibition of mouse group2A phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341250 | Inhibition of mouse group2V phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID158926 | Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC). | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives. |
| AID341252 | Inhibition of mouse group2X phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341246 | Inhibition of mouse group2E phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341244 | Inhibition of mouse group2D phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341239 | Inhibition of human group1B phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341237 | Inhibition of human group3 phospholipase-A2 at 1.6 uM | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341241 | Inhibition of human group2A phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341251 | Inhibition of human group2X phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341245 | Inhibition of human group2E phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341249 | Inhibition of human group2V phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID158925 | Inhibition of recombinant human secretory phospholipase A2 (sPLA2), chromogenic screening assay. | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives. |
| AID341240 | Inhibition of mouse group1B phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341247 | Inhibition of human group2F phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID341248 | Inhibition of mouse group2F phospholipase A2 fluorimetric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. |
| AID1894718 | Inhibition of human group IIA phospholipase A2 preincubated with compound for 10 mins followed by enzyme addition and measured after 30 mins by PC/DOC assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (20)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (10.00) | 18.2507 |
| 2000's | 15 (75.00) | 29.6817 |
| 2010's | 2 (10.00) | 24.3611 |
| 2020's | 1 (5.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 19.50
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.50) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (9.52%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 19 (90.48%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||