pelubiprofen: RN & structure given in first source; RN not in Chemline 3/84 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5282203 |
| CHEMBL ID | 69308 |
| SCHEMBL ID | 188062 |
| MeSH ID | M0120268 |
| Synonym |
|---|
| cs-670 |
| rs-2131 , |
| pelubiprofen |
| D01865 |
| 69956-77-0 |
| pelubiprofen (jan/inn) |
| CHEMBL69308 |
| NCGC00183010-01 |
| 2-[4-[(e)-(2-oxocyclohexylidene)methyl]phenyl]propanoic acid |
| dtxsid2048795 , |
| tox21_113272 |
| cas-69956-77-0 |
| dtxcid2028721 |
| cs 670 |
| 1619c79fvj , |
| unii-1619c79fvj |
| (+-)-p-(((e)-2-oxocyclohexylidene)methyl)hydratropic acid |
| 2-ocmpp |
| pelubiprofen [inn] |
| benzeneacetic acid, alpha-methyl-4-((2-oxocyclohexylidene)methyl)- |
| pelubiprofen [jan] |
| benzeneacetic acid, .alpha.-methyl-4-((2-oxocyclohexylidene)methyl)-, (e)- |
| pelubiprofen [who-dd] |
| SCHEMBL188062 |
| DB12150 |
| dw330sr |
| compound 13b [pmid: 6607354] |
| dw-330sr |
| gtpl9876 |
| CS-0011235 |
| HY-12383 |
| Q27251763 |
| EN300-21702735 |
| 2-(4-{[(1e)-2-oxocyclohexylidene]methyl}phenyl)propanoic acid |
| Z2583154614 |
| AKOS040742383 |
Pelubiprofen is a novel nonsteroidal anti-inflammatory, analgesic, and antipyretic drug. It has relatively selective effects on cyclooxygenase-2 activity.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pelubiprofen is a prodrug of 2-arylpropionic acid with relatively selective effects on cyclooxygenase-2 activity. " | ( Comparison of the efficacy and safety profiles of a pelubiprofen versus celecoxib in patients with rheumatoid arthritis: a 6-week, multicenter, randomized, double-blind, phase III, non-inferiority clinical trial. Baek, HJ; Cho, CS; Choi, IA; Chung, WT; Kang, SW; Kim, HA; Lee, J; Lee, SS; Lee, YA; Lee, YJ; Park, YB; Park, YE; Song, JS; Song, YW; Yoo, WH, 2014) | 2.1 |
| "Pelubiprofen is a novel nonsteroidal anti-inflammatory, analgesic, and antipyretic drug with at least similar efficacy and better tolerability compared with other nonsteroidal anti-inflammatory, analgesic, and antipyretic drugs such as naproxen and aceclofenac. " | ( Pharmacokinetic Interactions Between Pelubiprofen and Eperisone Hydrochloride: A Randomized, Open-label, Crossover Study of Healthy Korean Men. Chung, EK; Kim, HS; Kim, JI; Lee, KT; Noh, GJ; Ryu, JH, 2017) | 2.17 |
Pelubiprofen CR 90 mg is as effective as aceclofenac 200 mg with reduced adverse events for the treatment of symptomatic knee osteoarthritis.
No clinically significant changes were noted in the pharmacokinetic interactions of pelubiprofen and eperisone hydrochloride between monotherapy and combination therapy.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Excerpt | Relevance | Reference |
|---|---|---|
| "The present study aimed to develop the sustained-release oral dosage form of pelubiprofen (PEL) by using the blended mixture of 3-aminopropyl functionalized-magnesium phyllosilicate (aminoclay) and pH-independent polymers." | ( Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization. Han, HK; Lee, SH; Lee, YS; Song, JG, 2017) | 0.96 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 23.5187 | 0.0072 | 15.7588 | 89.3584 | AID1224835; AID624030 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 17.1505 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| AR protein | Homo sapiens (human) | Potency | 13.7282 | 0.0002 | 21.2231 | 8,912.5098 | AID743042; AID743054 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 28.7568 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 12.9614 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 23.9145 | 0.0008 | 17.5051 | 59.3239 | AID1159527 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 10.6845 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 11.8832 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 20.8575 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743075; AID743079; AID743080; AID743091 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 23.6719 | 0.0010 | 19.4141 | 70.9645 | AID743094; AID743140 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 8.4127 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 10.5909 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 23.7101 | 0.0016 | 28.0151 | 77.1139 | AID1259385 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 28.2263 | 0.0376 | 17.0823 | 61.1927 | AID1259364; AID1259388 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 29.0122 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 16.7855 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 26.6032 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 16.7855 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 16.7855 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
| Ataxin-2 | Homo sapiens (human) | Potency | 16.7855 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID182609 | Antiinflammatory activity on peroral administration against carrageenan paw edema | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID179639 | Antiinflammatory activity on peroral administration against carrageenan induced rat paw edema. | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID179638 | Antiinflammatory activity on peroral administration against adjuvant arthritis in rat. | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID178496 | Antiinflammatory activity on peroral administration in rat determined by Randall-Slelitto test | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID76665 | Antipyretic activity on peroral administration against LPS-induced fever in guinea pig. | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID179451 | Analgesic activity on peroral administration against Scald induced pain in rat paw | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID182814 | Gastric lesion activity on peroral administration in rat. | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| AID177772 | Analgesic activity on peroral administration against Bradykinin induced pain in rat paw | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (8.33) | 18.7374 |
| 1990's | 4 (16.67) | 18.2507 |
| 2000's | 1 (4.17) | 29.6817 |
| 2010's | 8 (33.33) | 24.3611 |
| 2020's | 9 (37.50) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (39.33) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (20.83%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 1 (4.17%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 18 (75.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||