Page last updated: 2024-12-04

alrestatin

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Description

alrestatin: aldose reductase inhibitor; RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2120
CHEMBL ID63055
SCHEMBL ID450743
MeSH IDM0066060

Synonyms (120)

Synonym
AC-13697
HMS3266E14
BRD-K35498378-001-03-8
2-(1,3-dioxobenzo[de]isoquinolin-2-yl)acetic acid
(1,3-dioxo-1h-benzo[de]isoquinolin-2(3h)-yl)acetic acid
(1,3-dioxo-1h,3h-benzo[de]isoquinolin-2-yl)-acetic acid
DIVK1C_006762
SPECTRUM_001449 ,
BSPBIO_003360
IDI1_002167
alrestatino [inn-spanish]
alrestatinum [inn-latin]
2,3-dihydro-1,3-dioxo-1h-benz(de)isochiolin-2-essigsaeure
brn 0244370
1,3-dioxo-1h-benz(de)isoquinoline-2(3h)-acetate
1h-benz(de)isoquinoline-2(3h)-acetic acid, 1,3-dioxo-
nsc 299132
alrestatin [inn]
1,3-dioxo-1h-benz(de)isoquinoline-2(3h)-acetic acid
alrestatine [inn-french]
NCGC00024613-01
CBDIVE_001884
CBDIVE_003810
tocris-0485
BIO2_000412
BIO2_000892
CBDIVE_004382
nsc299132
51411-04-2
nsc-299132
BSPBIO_001144
SPECTRUM5_001248
DB02020
alrestatin
NCGC00024613-02
KBIOGR_000358
KBIO2_000484
KBIOSS_000484
KBIOGR_000484
KBIO2_004497
KBIO2_003052
KBIO3_000887
KBIO1_001706
KBIOSS_001929
KBIO2_001929
KBIO2_005620
KBIO3_002862
KBIO3_000888
KBIO2_007065
SPECPLUS_000666
SPECTRUM4_000089
SPECTRUM3_001880
NCGC00024613-04
NCGC00024613-03
2-{2,4-dioxo-3-azatricyclo[7.3.1.0;{5,13}]trideca-1(12),5,7,9(13),10-pentaen-3-yl}acetic acid
bdbm16415
chembl63055 ,
STK395007
HMS2092B18
HMS1990J05
AKOS000143709
ay-22284
HMS1792J05
HMS1362J05
F0863-0248
nsc-758180
nsc758180
pharmakon1600-01502053
dtxsid7045655 ,
dtxcid5025655
tox21_110913
cas-51411-04-2
alrestatinum
4-21-00-05562 (beilstein handbook reference)
alrestatine
unii-515dhk15lg
515dhk15lg ,
alrestatino
CCG-109865
FT-0630645
AB00052267-02
alrestatin [who-dd]
1h-benz(de)isoquinoline-2(3h)acetic acid, 1,3-dioxo-
S5803
SCHEMBL450743
NCGC00024613-06
tox21_110913_1
CS-4830
1,3-dioxo-1h-benz[de]isoquinoline-2(3h)-acetic acid
GCUCIFQCGJIRNT-UHFFFAOYSA-N
1,3-dioxo-1h-benz[d,e]isoquinoline-2(3h)-acetic acid
HY-B1202
HMS3403J05
AB00052267_03
2-[1,3-dioxo-1h-benzo[de]isoquinolin-2(3h)-yl]acetic acid
SR-01000597621-1
sr-01000597621
SR-01000597621-2
SBI-0051717.P003
2-(1,3-dioxo-1h-benzo[de]isoquinolin-2(3h)-yl)acetic acid ,
Q4735714
Z56756231
HMS3675O19
BS-16959
BCP28030
ay-22284 pound>> ay22284 pound>> ay 22284
EX-A2966
HMS3411O19
BRD-K35498378-001-05-3
HMS3866E03
mfcd00181399
D81785
A913189
51411-04-2 (free acid)
alrestatin free acid
EN300-235766
2-{2,4-dioxo-3-azatricyclo[7.3.1.0,5,13]trideca-1(13),5,7,9,11-pentaen-3-yl}acetic acid
BCA41104
2-{2,4-dioxo-3-azatricyclo[7.3.1.0?,??]trideca-1(13),5,7,9,11-pentaen-3-yl}acetic acid
AC-35588

Research Excerpts

Overview

Alrestatin sodium is an effective inhibitor of gastric acid secretion and ulcer formation in the rat.

ExcerptReferenceRelevance
"Alrestatin sodium is an effective inhibitor of gastric acid secretion and ulcer formation in the rat."( Alrestatin: gastric acid antisecretory-antiulcer activity in the rat.
Borella, LE; Lippmann, W; Pugsley, TA; Seethaler, K, 1978
)
2.42

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID886; AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency22.38720.177814.390939.8107AID2147
15-lipoxygenase, partialHomo sapiens (human)Potency0.15850.012610.691788.5700AID887
RAR-related orphan receptor gammaMus musculus (house mouse)Potency10.59090.006038.004119,952.5996AID1159523
Microtubule-associated protein tauHomo sapiens (human)Potency0.02510.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency29.04530.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency0.00670.531815.435837.6858AID504845
activating transcription factor 6Homo sapiens (human)Potency9.52050.143427.612159.8106AID1159516
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency35.48130.001815.663839.8107AID894
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)1.50000.00041.877310.0000AID34795; AID34961
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC50 (µMol)56.30000.00101.191310.0000AID34646; AID34650; AID34651; AID34653; AID34654
Aldo-keto reductase family 1 member B1Homo sapiens (human)Ki4.75000.01903.41939.3000AID1797503
Aldo-keto reductase family 1 member B1Bos taurus (cattle)IC50 (µMol)6.35000.00702.589210.0000AID34503; AID34505
Peptidyl-prolyl cis-trans isomerase ESS1Saccharomyces cerevisiae S288CIC50 (µMol)10.00002.50002.50002.5000AID1799484
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
retinoid metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
epithelial cell maturationAldo-keto reductase family 1 member B1Homo sapiens (human)
renal water homeostasisAldo-keto reductase family 1 member B1Homo sapiens (human)
carbohydrate metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
C21-steroid hormone biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
L-ascorbic acid biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
regulation of urine volumeAldo-keto reductase family 1 member B1Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
negative regulation of apoptotic processAldo-keto reductase family 1 member B1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
fructose biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
cellular hyperosmotic salinity responseAldo-keto reductase family 1 member B1Homo sapiens (human)
metanephric collecting duct developmentAldo-keto reductase family 1 member B1Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member B1Bos taurus (cattle)
prostaglandin metabolic processAldo-keto reductase family 1 member B1Bos taurus (cattle)
retinol metabolic processAldo-keto reductase family 1 member B1Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
retinal dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member B1Homo sapiens (human)
electron transfer activityAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glyceraldehyde oxidoreductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
L-glucuronate reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member B1Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
extracellular spaceAldo-keto reductase family 1 member B1Homo sapiens (human)
nucleoplasmAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (102)

Assay IDTitleYearJournalArticle
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID398938Inhibition of rat lens aldose reductase at 10 uM
AID398937Inhibition of rat lens aldose reductase at 1 uM
AID34503In vitro inhibition of partially purified calf lens aldose reductase; value ranges from 10E-5 to 10E-61988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID329125Inhibition of Vibrio cholerae wild type ToxT-mediated transcription of ctx promoter at 50 uM2007Proceedings of the National Academy of Sciences of the United States of America, Feb-13, Volume: 104, Issue:7
Virstatin inhibits dimerization of the transcriptional activator ToxT.
AID34961Inhibitory activity against purified rat lens aldose reductase (RLAR)1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Molecular modeling studies of aldose reductase inhibitors.
AID34654Inhibitory activity against human placental aldose reductase in Sepharose 4B column at time 11985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID35115Inhibition of rat lens aldose reductase at 50 uM1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Isoxazolidine-3,5-diones as lens aldose reductase inhibitors.
AID34498Ability to cause 50% reduction in sorbitol levels of sciatic nerve of streptozotocinized rats was determined1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID26074pKa in DMF/H2O was measured1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID398936Inhibition of rat lens aldose reductase at 0.1 uM
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID34653Inhibitory activity against human placental aldose reductase in Sepharose 4B column at day 71985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID18149650% reduction in sorbitol accumulation in isolated sciatic nerves incubated in the presence of high glucose concentration1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID34651Inhibitory activity against human placental aldose reductase in Orange A column at time 21985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID173584Dose that decreased sorbitol accumulation by 50% in the sciatic nerve in the galactosemic rat model after administration for 3 weeks in the diet1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor.
AID34505Inhibition of bovine lens aldose reductase with DL-glyceraldehyde as substrate1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor.
AID173582Dose that decreased galactitol accumulation by 50% in the sciatic nerve in the galactosemic rat model after administration for 4 days in the diet1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor.
AID177563Ability to cause 50% reduction in sorbitol levels of sciatic nerve of streptozotocinized rats was determined; value ranges from 250-5001988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID176729Dose causing 50% reduction in sorbitol accumulation in isolated sciatic nerves of streptozotocinized rats, (tid)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID34646Inhibitory activity against human placental aldose reductase in 30 -70% (NH4)2SO4.1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID34650Inhibitory activity against human placental aldose reductase in Orange A column at day 81985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID233810The ratio of the inhibitory concentration causing a 50% reduction of sorbitol in the isolated nerve to the IC50 in the isolated enzyme1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID34795Inhibition of crude aldose reductase of rat lens1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1799484Pin1 Inhibition Assay from Article 10.1016/S1074-5521(02)00310-1: \\Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation.\\2003Chemistry & biology, Jan, Volume: 10, Issue:1
Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation.
AID1797503Enzyme Inhibition Assay from Article 10.1016/j.bioorg.2006.09.004: \\Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.\\2006Bioorganic chemistry, Dec, Volume: 34, Issue:6
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (47)

TimeframeStudies, This Drug (%)All Drugs %
pre-199019 (40.43)18.7374
1990's8 (17.02)18.2507
2000's5 (10.64)29.6817
2010's8 (17.02)24.3611
2020's7 (14.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.86

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.

MetricThis Compound (vs All)
Research Demand Index23.86 (24.57)
Research Supply Index4.08 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (9.43%)5.53%
Reviews6 (11.32%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other42 (79.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]