Compounds > ameltolide
Page last updated: 2024-12-05

ameltolide

Description

Ameltolide is a natural product isolated from the marine sponge *Aplysina aerophoba*. It exhibits potent anti-inflammatory and analgesic activity, making it a promising lead compound for drug development. Ameltolide is a highly oxygenated macrolide with a complex structure, posing a challenge for its synthetic production. Research into ameltolide focuses on understanding its biological activity, developing efficient synthetic routes for its production, and exploring its potential therapeutic applications.'

ameltolide: structure given in first source; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID13086
CHEMBL ID22916
CHEBI ID6342
SCHEMBL ID635392
MeSH IDM0155818

Synonyms (46)

Synonym
4-amino-n-(2,6-dimethylphenyl)benzamide
add-75073
ly-201116
ameltolide (usan/inn)
D02892
ameltolidum [inn-latin]
benzamide, 4-amino-n-(2,6-dimethylphenyl)-
ameltolide [usan:inn:ban]
4-amino-2',6'-benzoxylidide
brn 2734562
add 75073
ameltolida [inn-spanish]
ly 201116
2',6'-benzoxylidide, 4-amino-
STK360030
787-93-9
ly201116
ameltolide
chebi:6342 ,
CHEMBL22916
AKOS000136947
ameltolida
ameltolidum
f83240zove ,
unii-f83240zove
SCHEMBL635392
4-amino-n-(2,6-dimethyl-phenyl)-benzamide
HZIWGOAXOBPQGY-UHFFFAOYSA-N
4-amino-n-(2,6-dimethylphenyl) benzamide
tox21_113872
NCGC00253759-01
dtxcid4031271
dtxsid7052860 ,
cas-787-93-9
ameltolide [usan]
ameltolide [inn]
mfcd00865288
SR-01000944824-1
sr-01000944824
Q4742349
Z111686304
4-amino-n-(2,6-dimethylphenyl)benzamide 95%
ly 201116;add 75073
BS-36184
EN300-14405055
F87563

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" 14C-LY201116 was well absorbed (approximately 94%) from the gastrointestinal tract following oral administration."( Metabolism, disposition, and pharmacokinetics of a potent anticonvulsant, 4-amino-N-(2,6-dimethylphenyl)benzamide (LY201116), in rats.
Gabriel, S; Parli, CJ; Potts, BD, )		0.13

Dosage Studied

ExcerptRelevanceReference
" Naturally mated rats and rabbits were dosed once daily by gavage on gestation days (GD) 6-17 and 6-18, respectively."( Ameltolide. I: Developmental toxicology studies of a novel anticonvulsant.
Higdon, GL; Markham, JK; McKinley, ER, 1991)		1.72
" Dose-response and time-response studies for efficacy and rotorod toxicity were completed following intraperitoneal injection of the drug."( The effects of LY-201116 [4-amino-N-(2,6-dimethylphenyl) benzamide] on the amygdala-kindled rat.
Albertson, TE; Stark, LG, 1990)		0.28
" Two hr after oral dosing with 14C-LY201116, ADMP and HADMP comprised 92% of the total radioactivity in the plasma."( Metabolism, disposition, and pharmacokinetics of a potent anticonvulsant, 4-amino-N-(2,6-dimethylphenyl)benzamide (LY201116), in rats.
Gabriel, S; Parli, CJ; Potts, BD, )		0.13
" Initial screening in mice dosed intraperitoneally and rats dosed orally indicated that 4-AEPB is active against maximal electroshock-induced seizures (MES), but does not protect animals against subcutaneous pentylenetetrazole (sc Ptz)-induced seizures."( Anticonvulsant and neurotoxicological properties of 4-amino-N-(2-ethylphenyl)benzamide, a potent ameltolide analogue.
Bourhim, M; Diouf, O; Lambert, DM; Poupaert, JH; Stables, JP; Vamecq, J, 1997)		0.51
" Anticonvulsant ED50s (effective doses in at least 50% of animals tested) of compounds in the MES test were determined in rats dosed orally and amounted to 52 (1), 135 (2), 284 (3), 231 (8), 131 (9), 25 (10), 369 (13), 354 (14), and 121 (PHT) micromol/kg, compound 5 presenting with an ED50 value higher than 650 micromol/kg."( Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
Lambert, D; Masereel, B; Poupaert, JH; Stables, JP; Vamecq, J, 1998)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzamides
[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 (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.60320.006038.004119,952.5996AID1159521
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency27.54040.01237.983543.2770AID1645841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (77)

Assay IDTitleYearJournalArticle
AID109704Plasma concentration was determined after 30 min of oral administration in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID121848Compound for toxicity by rotarod assay method in mice after administration1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Anticonvulsant activity of 2- and 3-aminobenzanilides.
AID114484Compound for anticonvulsant activity against maximal electroshock (MES)-induced seizures in mice after administration1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Anticonvulsant activity of 2- and 3-aminobenzanilides.
AID226934Protective index measured as the ratio of HS ED50/MES ED50 values.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant.
AID119857Effect on Hexobarbitol-Induced sleeping time in mice at a dose of 3.2 mg/kg peroral administration1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID122454Time to peak anticonvulsant effect was measured after oral dosing in mice.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant.
AID119744Effect on Hexobarbitol-Induced sleeping time in mice at a dose of 12.8 mg/kg peroral administration1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID119742Effect on Hexobarbitol-Induced sleeping time in mice at a dose of 0 mg/kg peroral administration1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID119743Effect on Hexobarbitol-Induced sleeping time in mice at a dose of 1.6 mg/kg peroral administration1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID168763Anticonvulsant activity was determined in rats at a dose of 30 mg/kg after 4 hour by MES test. (++++ denotes activity in 75-100% of administered animals)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109361Anticonvulsant activity determined at 4 hours after the administration of compound using sc Ptz test.(- denotes activity at 300 mg/kg)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109703Plasma concentration was determined after 240 min of oral administration in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID123259Toxicity tested by rotarod test for neurologic deficit at interval of 30 min when 30 mg/kg was administered intraperitoneally; shows activity1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID197266In vivo anticonvulsant activity to prevent seizures from maximum electroshock (MES) in rat hippocampal slices2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID109702Plasma concentration was determined after 120 min of oral administration in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID109357Anticonvulsant activity determined at 4 hours after the administration of compound using MES test.(++= signify activity at 100 mg/kg)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID123264Toxicity tested by rotarod test for neurologic deficit at interval of 4 hr when 100 mg/kg was administered intraperitoneally; shows activity1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID122018Toxic dose was determined by the rotarod test in mice; activity value ranges from 13.27-16.881985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID226533Protective index measured as the ratio between TD50 and ED501986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Anticonvulsant activity of 2- and 3-aminobenzanilides.
AID168750Anticonvulsant activity was determined in rats at a dose of 30 mg/kg after 15 minutes by MES test. (++++ denotes activity in 75-100% of administered animals)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109366Anticonvulsant activity of 30 mg/kg after 30 min. of intraperitoneal administration in mice against maximum electroshock seizures (MES); compound shows activity1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID109706Plasma concentration was determined after 60 min of oral administration in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID114328Ataxia or neurological deficit was measured as horizontal screen test(HS) in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID226514Protective index (HS ED50/MES ED50) after oral administration in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID109345Anticonvulsant activity determined at 30 minutes after the administration of compound using MES test. (+++ = activity at 30 mg/kg)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID113256Antagonistic activity against MES (Maximal Electroshock)-induced seizures after oral administration to mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID113994Effective dose evaluated against maximal electric seizures (MES) or convulsions in mice; activity value ranges from 2.18-3.071985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID178278Anticonvulsant ED50 activity by MES test in rats dosed orally1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID212512Toxicity was determined in rats at a dose of 30 mg/kg after 4 hour. (- denotes no activity in administered animals).1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109370Anticonvulsant activity of 300 mg/kg of compound against subcutaneous induced metrazole convulsions at interval of 4 hr administered intraperitoneally in mice; no activity1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID168758Anticonvulsant activity was determined in rats at a dose of 30 mg/kg after 30 minutes by MES test. (++++ denotes activity in 75-100% of administered animals)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109352Anticonvulsant activity determined at 30 minutes after the administration of compound using sc Ptz test.(- denotes activity at 300 mg/kg)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID211678Neurotoxicity determined at 30 minutes after the administration of compound by rotarod test.(- denotes activity at 300 mg/kg)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID122340Time taken for peak anticonvulsant effect(TPE) was measured by oral administration to mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID211683Neurotoxicity determined at 4 hours after the administration of compound by rotarod test(- denotes activity at 300 mg/kg)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109705Plasma concentration was determined after 360 min of oral administration in mice1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID114132Anticonvulsant effect by maximal electroshock assay in mice after intravenous administration.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant.
AID205272Apparent IC50 value by [3H]batrachotoxinin-A-20-alpha-benzoate-binding test performed in rat brain synaptosomes1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID114130Anticonvulsant effect by horizontal screen assay in mice after peroral administration.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant.
AID119860Effect on Hexobarbitol-Induced sleeping time in mice at a dose of 6.4 mg/kg peroral administration1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Discovery and anticonvulsant activity of the potent metabolic inhibitor 4-amino-N-(2,6-dimethylphenyl)-3,5-dimethylbenzamide.
AID226534Protective index as the ratio of TD50 value against MES to that of ED50 value against MES.1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID109369Anticonvulsant activity of 300 mg/kg of compound against subcutaneous induced metrazole convulsions at interval of 30 min administered intraperitoneally in mice; no activity1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID168754Anticonvulsant activity was determined in rats at a dose of 30 mg/kg after 2 hour by MES test. (++++ denotes activity in 75-100% of administered animals)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID109367Anticonvulsant activity of 30 mg/kg after 4 hr of intraperitoneal administration in mice against maximum electroshock seizures (MES); compound shows activity1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Anticonvulsant activity of some 4-aminobenzanilides.
AID114134Anticonvulsant effect by maximal electroshock assay in mice after peroral administration.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant.
AID168604Anticonvulsant activity was determined in rats at a dose of 30 mg/kg after 1 hour by MES test. (++++ denotes activity in 75-100% of administered animals)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (16.67)18.7374
1990's8 (33.33)18.2507
2000's4 (16.67)29.6817
2010's2 (8.33)24.3611
2020's6 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other28 (96.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.0210amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
phenytoin
[no description available]		4.6990imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		3.110aromatic ether;
nitrile;
polyether;
tertiary amino compound
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		3.110dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carvedilol
[no description available]		3.110carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		2.3720branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
lidocaine
Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.		3.110benzenes;
monocarboxylic acid amide;
tertiary amino compound		anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
lamotrigine
[no description available]		3.1101,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
lomerizine
lomerizine: used to treat migraines		3.110diarylmethane
mexiletine
Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.		3.110aromatic ether;
primary amino compound		anti-arrhythmia drug
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		2.6630barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		3.110benzothiazoles
thalidomide
Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.		1.9910phthalimides;
piperidones
zonisamide
Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.		3.1101,2-benzoxazoles;
sulfonamide		anticonvulsant;
antioxidant;
central nervous system drug;
protective agent;
T-type calcium channel blocker
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		1.9910organic heterobicyclic compound;
organonitrogen heterocyclic compound
adamantane
Adamantane: A tricyclo bridged hydrocarbon.		1.9910adamantanes;
polycyclic alkane
remacemide
remacemide: structure given in first source		3.110stilbenoid
besipirdine
besipirdine: structure given in first source; a non-receptor-dependent cholinomimetic agent with noradrenergic activity with potential use for treating Alzheimer's disease		3.110
sipatrigine
sipatrigine: a glutamate release inhibitor which protects against focal cerebral ischemic damage		3.110pyrimidines
lubeluzole
lubeluzole: a benzothiazole compound; used for the treatment of acute ischemic stroke; R-91154 is the inactive isomer		3.110benzothiazoles
2,6-dimethylphenylphthalimide
2,6-dimethylphenylphthalimide: enhances alpha-tumor necrosis factor production; structure in first source		1.9910
4-amino-n-(2,6-dimethylphenyl)phthalimide
4-amino-N-(2,6-dimethylphenyl)phthalimide: a potent anticonvulsant against maximal electroshock-induced seizures; structure given in first source		3.520
ly 188544
LY 188544: RN given refers to cpd without isomeric designation; LY 188545 is the (S)-isomer; LY 188546 is the (R)-isomer; structure given in first source		2.3720benzamides
5-aminocarbonyl-10,11-dihydro-5h-dibenzo(a,d)cyclohepten-5,10-imine
5-aminocarbonyl-10,11-dihydro-5H-dibenzo(a,d)cyclohepten-5,10-imine: structure given in first source; n-methyl aspartate antagonist		3.110
flunarizine
Flunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.		3.110diarylmethane
irampanel
irampanel: structure in first source		3.110
topiramate
Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.		3.110cyclic ketal;
ketohexose derivative;
sulfamate ester		anticonvulsant;
sodium channel blocker
fmrfamide
FMRFamide: A molluscan neuroactive peptide which induces a fast excitatory depolarizing response due to direct activation of amiloride-sensitive SODIUM CHANNELS. (From Nature 1995; 378(6558): 730-3)		2.0210
batrachotoxinin a 20-alpha-benzoate
[no description available]		1.9910
ConditionIndicatedRelationship StrengthStudiesTrials
Absence Seizure
[description not available]		03.5990
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		03.5990
Apoplexy
[description not available]		02.9210
ALS - Amyotrophic Lateral Sclerosis
[description not available]		02.9210
Aura
[description not available]		02.9210
Amyotrophic Lateral Sclerosis
A degenerative disorder affecting upper MOTOR NEURONS in the brain and lower motor neurons in the brain stem and SPINAL CORD. Disease onset is usually after the age of 50 and the process is usually fatal within 3 to 6 years. Clinical manifestations include progressive weakness, atrophy, FASCICULATION, hyperreflexia, DYSARTHRIA, dysphagia, and eventual paralysis of respiratory function. Pathologic features include the replacement of motor neurons with fibrous ASTROCYTES and atrophy of anterior SPINAL NERVE ROOTS and corticospinal tracts. (From Adams et al., Principles of Neurology, 6th ed, pp1089-94)		02.9210
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.9210
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		02.9210
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Acute Liver Injury, Drug-Induced
[description not available]		02.0210
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		02.0210
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.3820
Abnormalities, Drug-Induced
Congenital abnormalities caused by medicinal substances or drugs of abuse given to or taken by the mother, or to which she is inadvertently exposed during the manufacture of such substances. The concept excludes abnormalities resulting from exposure to non-medicinal chemicals in the environment.		01.9710
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		01.9710
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