Page last updated: 2024-12-08
ertiprotafib
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
ertiprotafib: a hypoglycemic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 157049 |
| CHEMBL ID | 184041 |
| SCHEMBL ID | 6703442 |
| MeSH ID | M0482462 |
Synonyms (32)
| Synonym |
|---|
| ertiprotafib (usan/inn) |
| D04050 |
| 251303-04-5 |
| ertiprotafib |
| CHEMBL184041 , |
| ptp-112 |
| 2-[4-(9-bromo-2,3-dimethyl-naphtho[2,3-b]thiophen-4-yl)-2,6-dimethyl-phenoxy]-3-phenyl-propionic acid |
| bdbm50209683 |
| (r)-2-(4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thiophen-4-yl)-2,6-dimethylphenoxy)-3-phenylpropanoic acid |
| (2r)-2-[4-(9-bromo-2,3-dimethylbenzo[f][1]benzothiol-4-yl)-2,6-dimethylphenoxy]-3-phenylpropanoic acid |
| (2r)-2-(4-(9-bromo-2,3-dimethylnaphtho(2,3-b)thiophen-4-yl)-2,6-dimethylphenoxy)-3-phenylpropionic acid |
| ertiprotafib [usan:inn] |
| benzenepropanoic acid, alpha-(4-(9-bromo-2,3-dimethylnaphtho(2,3-b)thien-4-yl)-2,6-dimethylphenoxy)-, (alphar)- |
| benzenepropanoic acid, alpha-(4-(9-bromo-2,3-dimethylnaphtho(2,3-b)thien-4-yl)-2,6-dimethylphenoxy)-,(alpha r)- |
| 5tpm2eb426 , |
| (2r)-2-(4-(9-bromo-2,3-dimethylnaphtho(2,3-b)thiophen-4-yl)-2,6-dimethylphenoxy)-3-phenylpropionic acid |
| unii-5tpm2eb426 |
| benzenepropanoic acid, .alpha.-(4-(9-bromo-2,3-dimethylnaphtho(2,3-b)thien-4-yl)-2,6-dimethylphenoxy)-, (.alpha.r)- |
| ertiprotafib [inn] |
| ertiprotafib [usan] |
| (2r)-2-[4-(9-bromo-2,3-dimethylnaphtho[2,3-b]thiophen-4-yl)-2,6-dimethylphenoxy]-3-phenylpropionic acid |
| SCHEMBL6703442 |
| FONCZICQWCUXEB-RUZDIDTESA-N |
| (2r)-2-[4-(9-bromo-2,3-dimethyl-naphtho[2,3-b]thiophen-4-yl)-2,6-dimethyl-phenoxy]-3-phenyl-propionic acid |
| DTXSID30179814 |
| ptp112 |
| CS-0015482 |
| HY-19383 |
| DB06521 |
| Q27262858 |
| MS-30174 |
| AKOS040741711 |
Research Excerpts
Overview
Ertiprotafib is a PTP1B inhibitor that reached the clinical trial stage for the treatment of diabetes.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ertiprotafib is a PTP1B inhibitor that reached the clinical trial stage for the treatment of diabetes." | ( The mode of action of the Protein tyrosine phosphatase 1B inhibitor Ertiprotafib. Kumar, GS; Page, R; Peti, W, 2020) | 1.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Inhibitor of nuclear factor kappa-B kinase subunit beta | Homo sapiens (human) | IC50 (µMol) | 0.4000 | 0.0009 | 0.9781 | 9.8200 | AID295637 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 1.1798 | 0.0005 | 3.4984 | 9.7600 | AID1206864; AID1328333; AID1657529; AID1773666; AID295185; AID295638; AID301108; AID429098; AID440905; AID593354; AID637349 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | Ki | 1.5000 | 0.1900 | 4.8327 | 9.6000 | AID295185 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (57)
Molecular Functions (22)
Ceullar Components (16)
Bioassays (18)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID593354 | Inhibition of PTP1B | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | Using small molecules to target protein phosphatases. |
| AID295638 | Inhibition of PTP1B | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta). |
| AID637346 | Transactivation of human full length PPARalpha expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition. |
| AID237332 | Calculated partition coefficient (clogP) | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Prospects for inhibitors of protein tyrosine phosphatase 1B as antidiabetic drugs. |
| AID637349 | Inhibition of PTB1B using pNPP as substrate after 30 mins | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition. |
| AID295637 | Inhibition of IKK-beta after 30 mins | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta). |
| AID301108 | Inhibition of PTP1B after 10 mins | 2007 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19 | 2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity. |
| AID637350 | Hypoglycemic activity in diabetic KK-Ay mouse model assessed as decrease in glucose level at 10 mg/kg, po qd for 4 days relative to untreated control | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition. |
| AID637348 | Transactivation of human full length PPARalpha expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay relative to WY14643 | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition. |
| AID637345 | Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition. |
| AID1657529 | Inhibition of human recombinant PTP1B (1 to 299 residues) expressed in Escherichia coli using pNPP as substrate preincubated for 30 mins followed by substrate addition and measured after every 30 secs for 15 mins | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | PTP1B-Inhibiting Branched-Chain Fatty Acid Dimers from |
| AID1328333 | Inhibition of PTP1B (unknown origin) | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Design and synthesis of new potent PTP1B inhibitors with the skeleton of 2-substituted imino-3-substituted-5-heteroarylidene-1,3-thiazolidine-4-one: Part I. |
| AID637347 | Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay relative to farglitazar | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition. |
| AID1773666 | Inhibition of human recombinant PTP1B (1 to 322 residues) expressed in Escherichia coli using pNPP as substrate preincubated with substrate for 10 mins followed by enzyme addition and measured for 10 mins by absorbance based analysis | 2021 | Journal of natural products, 09-24, Volume: 84, Issue:9 | Dual High-Resolution α-Glucosidase and PTP1B Inhibition Profiling Combined with HPLC-PDA-HRMS-SPE-NMR Analysis for the Identification of Potentially Antidiabetic Chromene Meroterpenoids from |
| AID429098 | Inhibition of PTP1B by pNPP hydrolase assay | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Structure-based virtual screening approach to identify novel classes of PTP1B inhibitors. |
| AID295185 | Inhibition of PTP1B after 10 mins | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Methylenedisalicylic acid derivatives: new PTP1B inhibitors that confer resistance to diet-induced obesity. |
| AID1206864 | Inhibition of recombinant human PTP1B (1 to 299) expressed in Escherichia coli using p-nitrophenyl phosphate as substrate | 2015 | Bioorganic & medicinal chemistry, Jun-15, Volume: 23, Issue:12 | Perspective: Tyrosine phosphatases as novel targets for antiplatelet therapy. |
| AID440905 | Inhibition of PTP1B | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (16)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 8 (50.00) | 29.6817 |
| 2010's | 5 (31.25) | 24.3611 |
| 2020's | 3 (18.75) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 24.97
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 (24.97) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (6.25%) | 5.53% |
| Reviews | 2 (12.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 13 (81.25%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||